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1
Al Badri, Yaqeen Nadheer, Cheng Shu Chaw, and Amal Ali Elkordy. "Insights into Asymmetric Liposomes as a Potential Intervention for Drug Delivery Including Pulmonary Nanotherapeutics." Pharmaceutics 15, no. 1 (January 15, 2023): 294. http://dx.doi.org/10.3390/pharmaceutics15010294.
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Liposome-based drug delivery systems are nanosized spherical lipid bilayer carriers that can encapsulate a broad range of small drug molecules (hydrophilic and hydrophobic drugs) and large drug molecules (peptides, proteins, and nucleic acids). They have unique characteristics, such as a self-assembling bilayer vesicular structure. There are several FDA-approved liposomal-based medicines for treatment of cancer, bacterial, and viral infections. Most of the FDA-approved liposomal-based therapies are in the form of conventional “symmetric” liposomes and they are administered mainly by injection. Arikace® is the first and only FDA-approved liposomal-based inhalable therapy (amikacin liposome inhalation suspension) to treat only adults with difficult-to-treat Mycobacterium avium complex (MAC) lung disease as a combinational antibacterial treatment. To date, no “asymmetric liposomes” are yet to be approved, although asymmetric liposomes have many advantages due to the asymmetric distribution of lipids through the liposome’s membrane (which is similar to the biological membranes). There are many challenges for the formulation and stability of asymmetric liposomes. This review will focus on asymmetric liposomes in contrast to conventional liposomes as a potential clinical intervention drug delivery system as well as the formulation techniques available for symmetric and asymmetric liposomes. The review aims to renew the research in liposomal nanovesicle delivery systems with particular emphasis on asymmetric liposomes as future potential carriers for enhancing drug delivery including pulmonary nanotherapeutics.
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Ishida, Tatsuhiro, Hideyoshi Harashima, and Hiroshi Kiwada. "Liposome Clearance." Bioscience Reports 22, no. 2 (April 1, 2002): 197–224. http://dx.doi.org/10.1023/a:1020134521778.
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The clearance rate of liposomal drugs from the circulation is determined by the rate and extent of both drug release and uptake of liposomes by cells of the mononuclear phagocyte system (MPS). Intravenously injected liposomes initially come into contact with serum proteins. The interaction of liposomes with serum proteins is thought to play a critical role in the liposome clearance. Therefore, in this review, we focus on the role of serum proteins, so-called opsonins, that enhance the clearance of liposomes, when bound to liposomes. In addition to opsonin-dependent liposome clearance, opsonin-independent liposome clearance is also reviewed. As opposed to the conventional (non-surface modification) liposomes, we briefly address the issue of the accelerated clearance of PEGylated-liposomes (sterically stabilized liposomes, long-circulating liposomes) on repeated injection, a process that has recently been observed.
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Cattel, Luigi, Maurizio Ceruti, and Franco Dosio. "From Conventional to Stealth Liposomes a new Frontier in Cancer Chemotherapy." Tumori Journal 89, no. 3 (May 2003): 237–49. http://dx.doi.org/10.1177/030089160308900302.
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Many attempts have been made to achieve good selectivity to targeted tumor cells by preparing specialized carrier agents that are therapeutically profitable for anticancer therapy. Among these, liposomes are the most studied colloidal particles thus far applied in medicine and in particular in antitumor therapy. Although they were first described in the 1960s, only at the beginning of 1990s did the first therapeutic liposomes appear on the market. The first-generation liposomes (conventional liposomes) comprised a liposome-containing amphotericin B, Ambisome (Nexstar, Boulder, CO, USA), used as an antifungal drug, and Myocet (Elan Pharma Int, Princeton, NJ, USA), a doxorubicin-containing liposome, used in clinical trials to treat metastatic breast cancer. The second-generation liposomes (“pure lipid approach”) were long-circulating liposomes, such as Daunoxome, a daunorubicin-containing liposome approved in the US and Europe to treat AIDS-related Kaposi's sarcoma. The third-generation liposomes were surface-modified liposomes with gangliosides or sialic acid, which can evade the immune system responsible for removing liposomes from circulation. The fourth-generation liposomes, pegylated liposomal doxorubicin, were called “stealth liposomes” because of their ability to evade interception by the immune system, in the same way as the stealth bomber was able to evade radar. Actually, the only stealth liposome on the market is Caelyx/Doxil (Schering-Plough, Madison NJ, USA), used to cure AIDS-related Kaposi's sarcoma, resistant ovarian cancer and metastatic breast cancer. Pegylated liposomal doxorubicin is characterized by a very long-circulation half-life, favorable pharmacokinetic behavior and specific accumulation in tumor tissues. These features account for the much lower toxicity shown by Caelyx in comparison to free doxorubicin, in terms of cardiotoxicity, vesicant effects, nausea, vomiting and alopecia. Pegylated liposomal doxorubicin also appeared to be less myelotoxic than doxorubicin. Typical forms of toxicity associated to it are acute infusion reaction, mucositis and palmar plantar erythrodysesthesia, which occur especially at high doses or short dosing intervals. Active and cell targeted liposomes can be obtained by attaching some antigen-directed monoclonal antibodies (Moab or Moab fragments) or small proteins and molecules (folate, epidermal growth factor, transferrin) to the distal end of polyethylene glycol in pegylated liposomal doxorubicin. The most promising therapeutic application of liposomes is as non-viral vector agents in gene therapy, characterized by the use of cationic phospholipids complexed with the negatively charged DNA plasmid. The use of liposome formulations in local-regional anticancer therapy is also discussed. Finally, pegylated liposomal doxorubicin containing radionuclides are used in clinical trials as tumor-imaging agents or in positron emission tomography.
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Yanagihara, Shin, Yukiya Kitayama, Eiji Yuba, and Atsushi Harada. "Preparing Size-Controlled Liposomes Modified with Polysaccharide Derivatives for pH-Responsive Drug Delivery Applications." Life 13, no. 11 (November 3, 2023): 2158. http://dx.doi.org/10.3390/life13112158.
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The liposome particle size is an important parameter because it strongly affects content release from liposomes as a result of different bilayer curvatures and lipid packing. Earlier, we developed pH-responsive polysaccharide-derivative-modified liposomes that induced content release from the liposomes under weakly acidic conditions. However, the liposome used in previous studies size was adjusted to 100–200 nm. The liposome size effects on their pH-responsive properties were unclear. For this study, we controlled the polysaccharide-derivative-modified liposome size by extrusion through polycarbonate membranes having different pore sizes. The obtained liposomes exhibited different average diameters, in which the diameters mostly corresponded to the pore sizes of polycarbonate membranes used for extrusion. The amounts of polysaccharide derivatives per lipid were identical irrespective of the liposome size. Introduction of cholesterol within the liposomal lipid components suppressed the size increase in these liposomes for at least three weeks. These liposomes were stable at neutral pH, whereas the content release from liposomes was induced at weakly acidic pH. Smaller liposomes exhibited highly acidic pH-responsive content release compared with those from large liposomes. However, liposomes with 50 mol% cholesterol were not able to induce content release even under acidic conditions. These results suggest that control of the liposome size and cholesterol content is important for preparing stable liposomes at physiological conditions and for preparing highly pH-responsive liposomes for drug delivery applications.
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Kumar, Amit, Madhu Gupta, and Simran Braya. "Liposome Characterization, Applications and Regulatory landscape in US." International Journal of Drug Regulatory Affairs 9, no. 2 (June 22, 2021): 81–89. http://dx.doi.org/10.22270/ijdra.v9i2.474.
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Liposomes are lipid based drug carrier whose therapeutic performance depends on their structure. Liposomes offer several advantages over the conventional drug like target drug delivery, reduced toxicity, and extended pharmacokinetics. Characterization and Identification of critical attribute of liposomal formulation and suitable strategies for control during product development is important for quality of the liposomal drug product. This paper discusses the current status of the liposomal drug product and strategy used in regulating liposome product. Despite of lack of regulatory guidelines many liposome formulations get approved which shows the potential of liposome drug products.
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Goins, Beth A., and William T. Phillips. "The Use of Scintigraphic Imaging During Liposome Drug Development." Journal of Pharmacy Practice 14, no. 5 (October 2001): 397–406. http://dx.doi.org/10.1106/da2m-fyju-1xxq-ppkk.
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Liposomes, spherical lipid bilayers enclosing an aqueous space, have become an important class of drug carriers. This review describes the usefulness of scintigraphic imaging during the development of liposome-based drugs. This imaging modality is particularly helpful for tracking the distribution of liposomes in the body, monitoring the therapeutic responses following administration of liposome-based drugs, and investigating the physiological responses associated with liposome administration. Scintigraphy also can be used to monitor the therapeutic responses of patients given approved liposomal drugs. Several examples describing the potential of this imaging modality during both the preclinical formulation and clinical trial stages of liposomal drug development are included. Techniques for radiolabeling liposomes as well as methods for producing scintigraphic images are also described.
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Marqués-Gallego, Patricia, and Anton I. P. M. de Kroon. "Ligation Strategies for Targeting Liposomal Nanocarriers." BioMed Research International 2014 (2014): 1–12. http://dx.doi.org/10.1155/2014/129458.
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Liposomes have been exploited for pharmaceutical purposes, including diagnostic imaging and drug and gene delivery. The versatility of liposomes as drug carriers has been demonstrated by a variety of clinically approved formulations. Since liposomes were first reported, research of liposomal formulations has progressed to produce improved delivery systems. One example of this progress is stealth liposomes, so called because they are equipped with a PEGylated coating of the liposome bilayer, leading to prolonged blood circulation and improved biodistribution of the liposomal carrier. A growing research area focuses on the preparation of liposomes with the ability of targeting specific tissues. Several strategies to prepare liposomes with active targeting ligands have been developed over the last decades. Herein, several strategies for the functionalization of liposomes are concisely summarized, with emphasis on recently developed technologies for the covalent conjugation of targeting ligands to liposomes.
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Al Mutairi, Amal Abdullah, and Mohsen Mahmoud Mady. "Biophysical Characterization of (DOX-NPtm): FTIR and DSC Studies." JOURNAL OF ADVANCES IN PHYSICS 20 (March 3, 2022): 41–47. http://dx.doi.org/10.24297/jap.v20i.9194.
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Doxorubicin loaded into liposomes grafted with polyethylene glycol (PEG) has been demonstrated to have a longer circulation time and lower cardiotoxicity than doxorubicin (DOX). This study aims to investigate the biophysical characterization of a marketed formulation DOX-encapsulated liposome (DOX-NPTM). The interactions between doxorubicin and liposomal lipids can help in liposomal development. The liposome and DOX-NPTM were characterized in terms of differential scanning calorimetry (DSC) and Fourier transform infrared spectroscopy (FTIR). The rheological properties of liposomal samples were also measured. Physical interactions may be occurred between the drug functional groups and liposomal lipids, probably by weak hydrogen bond formation or weak bond formation due to dipole-dipole interaction. There was no shift of existing peaks or appearance of new peaks was detected between the characteristic peaks of the liposomal lipids were present in the DOX-encapsulated liposome sample. This suggests that there were physical interactions that took place only between the drug and lipids and no chemical interaction between them. DSC information shows that the phase transition temperature shifts to lower temperature degrees after loading of DOX into the liposomes. The DSC curve has a small broadening. This may infer a little cooperativity decrease between acyl chains of liposomal membranes after DOX inclusion. The encapsulation of DOX into liposomes decreases the plastic viscosity of liposomes (from 1.64 to 1.48 cP), which shows that the membrane fluidity was increased.
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Abbase, Eman R., Medhat W. Shafaa, and Mohsen M. Mady. "Competition Between Heparin and Polyethylene Glycol as Biofunctionalization for Improving Stability of Liposomal Doxorubicin." Advanced Science, Engineering and Medicine 12, no. 2 (February 1, 2020): 271–77. http://dx.doi.org/10.1166/asem.2020.2496.
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In order to improve liposomal doxorubicin stability, differentiation between Heparin and Polyethylene Glycol (PEG) as biofunctionalization for liposomal doxorubicin has been investigated by measuring the entrapment efficiency, size distribution, zeta potential, evaluating the in vitro potential cytotoxicity against MCF-7 (Breast cancer cell) and stability in serum by measuring the drug release rate. We synthesized Four liposomal formulations: (A) Conventional liposomes; DPPC:DOX, (B) Positively charged PEGylated liposomes; DPPC:CHOL:SA:PEG:DOX (C) Negatively charged PEGylated liposomes: DPPC:CHOl:DCP:PEG:DOX (D) positively charged liposomes to conjugate heparin; DPPC:CHOL:SA:DOX. Entrapment efficiency of doxorubicin dramatically increased after PEGylation and conjugation with heparin. In addition, zeta potential was changed upon the encapsulation of doxorubicin into conventional and PEGylated liposomes which indicates that DOX encapsulated completely into liposomes. For heparin conjugated liposomes, zeta potential was slightly changed. Sulphorhodamine-B (SRB) assay showed a greater cytotoxic effect of the liposomal doxorubicin formulations at different concentrations with respect to free drug against MCF-7 cell lines. The anticancer activity order was observed between the various liposome formulations, especially those observed with conjugated heparin liposomes. Slower drug release rate showed an order of D > C > B > A that means stability showed an order of D > C > B > A. From above results, the most stable liposomal doxorubicin formulation was the liposomal formulation D. The results optimized using heparin than PEG as biofunctionalization. Further studies are suggested for better understanding why heparin improves the stability of liposomal doxorubicin.
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Heneweer, Carola, Tuula Peñate Medina, Robert Tower, Holger Kalthoff, Richard Kolesnick, Steven Larson, and Oula Peñate Medina. "Acid-Sphingomyelinase Triggered Fluorescently Labeled Sphingomyelin Containing Liposomes in Tumor Diagnosis after Radiation-Induced Stress." International Journal of Molecular Sciences 22, no. 8 (April 8, 2021): 3864. http://dx.doi.org/10.3390/ijms22083864.
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In liposomal delivery, a big question is how to release the loaded material into the correct place. Here, we will test the targeting and release abilities of our sphingomyelin-consisting liposome. A change in release parameters can be observed when sphingomyelin-containing liposome is treated with sphingomyelinase enzyme. Sphingomyelinase is known to be endogenously released from the different cells in stress situations. We assume the effective enzyme treatment will weaken the liposome making it also leakier. To test the release abilities of the SM-liposome, we developed several fluorescence-based experiments. In in vitro studies, we used molecular quenching to study the sphingomyelinase enzyme-based release from the liposomes. We could show that the enzyme treatment releases loaded fluorescent markers from sphingomyelin-containing liposomes. Moreover, the release correlated with used enzymatic activities. We studied whether the stress-related enzyme expression is increased if the cells are treated with radiation as a stress inducer. It appeared that the radiation caused increased enzymatic activity. We studied our liposomes’ biodistribution in the animal tumor model when the tumor was under radiation stress. Increased targeting of the fluorescent marker loaded to our liposomes could be found on the site of cancer. The liposomal targeting in vivo could be improved by radiation. Based on our studies, we propose sphingomyelin-containing liposomes can be used as a controlled release system sensitive to cell stress.
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Yaroslavov, Alexander A., and Andrey V. Sybachin. "Multifunctional carriers for controlled drug delivery." Pure and Applied Chemistry 92, no. 6 (June 25, 2020): 919–39. http://dx.doi.org/10.1515/pac-2019-1111.
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AbstractIn the review we describe a method for concentration of anionic liposomes with encapsulated water-soluble substances within a small volume via electrostatic liposome adsorption on the surface of polymer particles with grafted cationic chains (spherical polycationic brushes), or cationic microgel particles. Dozens of intact liposomes can be bound to each polymer particle, the resulting polymer/liposome complex does not dissociate into the original components in a physiological solution. This allows fabrication of multi-liposomal complexes (MLCs) with a required ratio of encapsulated substances. Two approaches are discussed for the synthesis of stimuli-sensitive MLCs. The first is to incorporate the conformation switch, morpholinocyclohexanol-based lipid, into the liposomal membrane thus forming pH-sensitive liposomes capable of releasing their cargo when acidifying the surrounding solution. These liposomes complexed with the brushes release encapsulated substances much faster than the uncomplexed liposomes. The second is to adsorb liposomes on cationic thermo-responsive microgels. The resulting MLCs contracts upon heating over a volume phase transition temperature from the swollen to the collapsed state of microgel, thus causing the adsorbed liposomes to change drastically their morphology and release an encapsulated substance. Complexation of anionic liposomes with chitosan microgels and polylactide micelles gives MLCs which degrade in the presence of enzymes down to small particles, 10–15 nm in diameter. A novel promising approach suggests that immobilized liposomes can act as a capacious depot for biologically active compounds and ensure their controllable leakage to surrounding solution.
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Debs, R. J., N. Düzgüneş, E. N. Brunette, B. Fendly, J. Patton, and R. Philip. "Liposome-associated tumor necrosis factor retains bioactivity in the presence of neutralizing anti-tumor necrosis factor antibodies." Journal of Immunology 143, no. 4 (August 15, 1989): 1192–97. http://dx.doi.org/10.4049/jimmunol.143.4.1192.
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Abstract Cell-associated TNF-alpha, either bound to its receptor on monocyte membranes or expressed as an integral membrane protein, can exert potent tumor cytolytic activity. We assessed the interaction of TNF with the lipid bilayer membrane system, liposomes, and the effects of membrane association on TNF bioactivity. High levels of TNF can be encapsulated within liposomes. At neutral pH, TNF binds to the surface of preformed liposomes (liposome-associated TNF), but does not partition into the lipid bilayer. TNF appears to bind to negatively charged phospholipid head groups of the outer membrane leaflet. Free TNF, liposome-associated TNF, and liposome-encapsulated TNF display comparable abilities to activate human peripheral blood monocytes and to lyse tumor cells. However, liposome-encapsulated TNF, as well as TNF bound to the outer surface of preformed liposomes, retains bioactivity in the presence of anti-TNF antibodies that neutralize free TNF. The interaction of liposomal TNF with cell surface TNF receptors thus appears to be preserved in the presence of neutralizing antibodies.
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Chavoshian, Omid, Mahdieh Arabsalmani, Mahmoud Reza Jaafari, Ali Khamesipour, Azam Abbasi, Zahra Saberi, and Ali Badiee. "A Phospholipase-A Activity in Soluble Leishmania Antigens Causes Instability of Liposomes." Current Drug Delivery 17, no. 9 (October 27, 2020): 806–14. http://dx.doi.org/10.2174/1567201817666200731164002.
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Aim: This study aimed to investigate the existence of phospholipase-A (PLA) activity in Soluble L. major Antigens (SLA) because of no reports for it so far. Liposomes were used as sensors to evaluate PLA activity. Objective: Liposomal SLA consisting of Egg Phosphatidylcholine (EPC) or Sphingomyelin (SM) were prepared by two different methods in different pH or temperatures and characterized by Dynamic Light Scattering (DLS) and Thin Layer Chromatography (TLC). Methods: Lipid hydrolysis led to the disruption of EPC liposomal SLA in both methods but the Film Method (FM) produced more stable liposomes than the Detergent Removal Method (DRM). Results: The preparation of EPC liposomal SLA at pH 6 via FM protected liposomes from hydrolysis to some extent for a short time. EPC liposomes but not SM liposomes were disrupted in the presence of SLA. Conclusion: Therefore, a phospholipid without ester bond such as SM should be utilized in liposome formulations containing PLA as an encapsulating protein.
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Hattori, Yoshiyuki, Masataka Date, Shohei Arai, Kumi Kawano, Etsuo Yonemochi, and Yoshie Maitani. "Transdermal Delivery of Small Interfering RNA with Elastic Cationic Liposomes in Mice." Journal of Pharmaceutics 2013 (December 26, 2013): 1–6. http://dx.doi.org/10.1155/2013/149695.
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We developed elastic cationic liposomal vectors for transdermal siRNA delivery. These liposomes were prepared with 1,2-dioleoyl-3-trimethylammonium-propane (DOTAP) as a cationic lipid and sodium cholate (NaChol) or Tween 80 as an edge activator. When NaChol or Tween 80 was included at 5, 10, and 15% (w/w) into DOTAP liposomal formulations (C5-, C10-, and C15-liposomes and T5-, T10-, and T15-liposomes), C15- and T10-liposomes showed 2.4- and 2.7-fold-higher elasticities than DOTAP liposome, respectively. Although the sizes of all elastic liposomes prepared in this study were about 80–90 nm, the sizes of C5-, C10- and C15-liposome/siRNA complexes (lipoplexes) were about 1,700–1,800 nm, and those of T5-, T10-, and T15-lipoplexes were about 550–780 nm. Their elastic lipoplexes showed strong gene suppression by siRNA without cytotoxicity when transfected into human cervical carcinoma SiHa cells. Following skin application of the fluorescence-labeled lipoplexes in mice, among the elastic lipoplexes, C15- and T5-lipoplexes showed effective penetration of siRNA into skin, compared with DOTAP lipoplex and free siRNA solution. These data suggest that elastic cationic liposomes containing an appropriate amount of NaChol or Tween 80 as an edge activator could deliver siRNA transdermally.
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Sandal, Pallavi, Galal Mohsen Hussein Alsayadi, Abhishek Verma, Yash Choudhary, and Balak Das Kurmi. "Liposomal drug delivery: Recent developments and challenges." Pharmaspire 14, no. 01 (2022): 41–46. http://dx.doi.org/10.56933/pharmaspire.2022.14105.
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The spherical vesicles known as liposomes may contain one or many phospholipid bilayers. The first liposomes were found in the 1960s. One of the many distinctive drug delivery methods is the liposome, which offers a complex way to transfer active molecules to the site of action. Clinical trials are now testing a variety of formulations. Long-lasting second-generation liposomes are created by altering the vesicle’s lipid composition, size, and charge. Superficial vesicles have given way to liposome growth. Glycolipids and other substances have been used to make liposomes for the modification of outer surfaces through various types of targeting ligands and detecting agents or moiety. Now, the liposomes developed for the different market and it is flooded with cosmetics and, more crucially, medications. Three of the main applications of liposome technology include steric and environmental stabilization of loaded molecules, remote drug loading through pH and ion gradients approach, and simultaneously lipoplexes which is the complexes forms of cationic liposomes with anionic nucleic acids or proteins for the gene delivery or siRNA technology. The scope of liposome research was expanded, allowing for the production of various goods. The present review focuses on the different aspects of liposomal drug delivery concerning types, preparation, pros, and cons.
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Glukhova, Olga E. "Liposome Drug Delivery System across Endothelial Plasma Membrane: Role of Distance between Endothelial Cells and Blood Flow Rate." Molecules 25, no. 8 (April 18, 2020): 1875. http://dx.doi.org/10.3390/molecules25081875.
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This paper discusses specific features of the interactions of small-diameter liposomes with the cytoplasmic membrane of endothelial cells using in silico methods. The movement pattern of the liposomal drug delivery system was modeled in accordance with the conditions of the near-wall layer of blood flow. Our simulation results show that the liposomes can become stuck in the intercellular gaps and even break down when the gap is reduced. Liposomes stuck in the gaps are capable of withstanding a shell deformation of ~15% with an increase in liposome energy by 26%. Critical deformation of the membrane gives an impetus to drug release from the liposome outward. We found that the liposomes moving in the near-wall layer of blood flow inevitably stick to the membrane. Liposome sticking on the membrane is accompanied by its gradual splicing with the membrane bilayer. This leads to a gradual drug release inside the cell.
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Umbarkar, Mahesh, Swapnil Thakare, Tanaji Surushe, Amol Giri, and Vaibhav Chopade. "Formulation and Evaluation of Liposome by Thin Film Hydration Method." Journal of Drug Delivery and Therapeutics 11, no. 1 (January 15, 2021): 72–76. http://dx.doi.org/10.22270/jddt.v11i1.4677.
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Liposomes are the most advance formulation for targeting and controlled drug delivery system. These liposomes are generally administered by intra-venous route. In this work the liposome was prepared by using thin film hydration method. The formulated liposome is evaluated or characterised by using zeta sizer, Encapsulation efficiency, Entrapment efficiency, In vitro drug release. Main things are drug which are used for formulation of liposome was Diclofenac sodium, it having anti-inflammatory and anti-pyretic effect. The Diclofenac sodium having several adverse effects, such as depression of renal function, Liver failure for repeated administration, Local mucosal irritation, gastritis. To avoid this adverse effect Diclofenac sodium are incorporate in liposomal formulation. By formulating liposomal formulation, the bioavailability of Diclofenac sodium increase. In conventional dosage form bioavailability of diclofenac sodium is 50℅. But in liposomal formulation bioavailability of this drug increase. The final result includes that diclofenac liposome formulation shows more sustained and prolong anti-inflammatory activity.
Keywords: Diclofenac sodium, Liposome, Anti-inflammatory activity.
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Jian, Cheng-Bang, Xu-En Yu, Hua-De Gao, Huai-An Chen, Ren-Hua Jheng, Chong-Yan Chen, and Hsien-Ming Lee. "Liposomal PHD2 Inhibitors and the Enhanced Efficacy in Stabilizing HIF-1α." Nanomaterials 12, no. 1 (January 3, 2022): 163. http://dx.doi.org/10.3390/nano12010163.
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Prolyl hydroxylase domain-containing protein 2 (PHD2) inhibition, which stabilizes hypoxia-inducible factor (HIF)-1α and thus triggers adaptation responses to hypoxia in cells, has become an important therapeutic target. Despite the proven high potency, small-molecule PHD2 inhibitors such as IOX2 may require a nanoformulation for favorable biodistribution to reduce off-target toxicity. A liposome formulation for improving the pharmacokinetics of an encapsulated drug while allowing a targeted delivery is a viable option. This study aimed to develop an efficient loading method that can encapsulate IOX2 and other PHD2 inhibitors with similar pharmacophore features in nanosized liposomes. Driven by a transmembrane calcium acetate gradient, a nearly 100% remote loading efficiency of IOX2 into liposomes was achieved with an optimized extraliposomal solution. The electron microscopy imaging revealed that IOX2 formed nanoprecipitates inside the liposome’s interior compartments after loading. For drug efficacy, liposomal IOX2 outperformed the free drug in inducing the HIF-1α levels in cell experiments, especially when using a targeting ligand. This method also enabled two clinically used inhibitors—vadadustat and roxadustat—to be loaded into liposomes with a high encapsulation efficiency, indicating its generality to load other heterocyclic glycinamide PHD2 inhibitors. We believe that the liposome formulation of PHD2 inhibitors, particularly in conjunction with active targeting, would have therapeutic potential for treating more specifically localized disease lesions.
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Gorbik, V. S., Z. S. Shprakh, Z. M. Kozlova, and V. G. Salova. "LIPOSOMES AS A TARGETED DELIVERY SYSTEM OF DRUGS (REVIEW)." Russian Journal of Biotherapy 20, no. 1 (April 8, 2021): 33–41. http://dx.doi.org/10.17650/1726-9784-2021-20-1-33-41.
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Liposomal targeted drug delivery makes it possible to achieve effective concentration in the target cell under various pathological conditions. The main advantage of liposomal particles is their biodegradability and immunological neutrality, which improves the safety profile of drugs. The review provides information on the composition of liposomes: the main component of the liposomal membrane is phospholipids, which provide its strength and protect from mechanical impacts. Liposomal particles are distinguished by the size and number of bilayer membranes, also secreted liposomes with a non‑lamellar organization. The composition and size of liposomes are selected depending on the purpose, including excipients in the membrane that affect the properties and functions of liposomes, including the rate of release of the components, the affinity of liposomes for the target tissue, etc. The review considers the main methods for obtaining liposomes and the features of their use, advantages and disadvantages. The creation of liposomes that are sensitive to various external or internal physicochemical factors makes it possible to realize drugs effects, localize the site of its action and reduce the number and severity of side effects. Currently, liposome‑based drugs are successfully used in various fields of medicine – dermatology, cardiology, oncology, neurology, etc. The most active condact preclinical and clinical studies of liposomal drugs for the treatment of malignant neoplasms. Particular attention is paid to the work of Russian researchers in the field of targeted drug delivery. It is shown that today liposomes are an open for study and improvement system for targeted drug delivery.
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Nalawade, Vishwajit, and Kunal Patil. "Liposome: A Novel Drug Delivery System." International Journal of Research Publication and Reviews 04, no. 01 (2022): 1795–801. http://dx.doi.org/10.55248/gengpi.2023.4148.
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Liposome was derived from two Greek words “Lipos meaning fat and Soma meaning body”. Liposome were spherical shaped vesicles consist of phospholipids and cholesterol. Due to their size hydrophobic and lipophilic character they are very promising system for drug delivery. This novel drug delivery system aims to target the drug directly to the site of action. Liposomes are very biocompatible and stable and have unique property to entrap both hydrophilic drug and lipophilic drug to its compartment and lead to controlled release effect. They are of 0.05- 5.0 micrometer in diameter. Liposomes are used for the treatment of various diseases like tumors or cancer. Liposomal Drug Delivery System and various aspects related to liposome that can be studied Compared with traditional drug delivery systems, liposomes exhibit better properties, including site-targeting, sustained or controlled release, protection of drugs from degradation and clearance, superior therapeutic effects, and lower toxic side effects. This review describes liposomes structure, composition, preparation methods, and evaluation clinical applications
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Kan, Pei, Chih-Wan Tsao, Ae-June Wang, Wu-Chou Su, and Hsiang-Fa Liang. "A Liposomal Formulation Able to Incorporate a High Content of Paclitaxel and Exert Promising Anticancer Effect." Journal of Drug Delivery 2011 (October 11, 2011): 1–9. http://dx.doi.org/10.1155/2011/629234.
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A liposome formulation for paclitaxel was developed in this study. The liposomes, composed of naturally unsaturated and hydrogenated phosphatidylcholines, with significant phase transition temperature difference, were prepared and characterized. The liposomes exhibited a high content of paclitaxel, which was incorporated within the segregated microdomains coexisting on phospholipid bilayer of liposomes. As much as 15% paclitaxel to phospholipid molar ratio were attained without precipitates observed during preparation. In addition, the liposomes remained stable in liquid form at 4 for at least 6 months. The special composition of liposomal membrane which could reduce paclitaxel aggregation could account for such a capacity and stability. The cytotoxicity of prepared paclitaxel liposomes on the colon cancer C-26 cell culture was comparable to Taxol. Acute toxicity test revealed that L for intravenous bolus injection in mice exceeded by 40 mg/kg. In antitumor efficacy study, the prepared liposomal paclitaxel demonstrated the increase in the efficacy against human cancer in animal model. Taken together, the novel formulated liposomes can incorporate high content of paclitaxel, remaining stable for long-term storage. These animal data also demonstrate that the liposomal paclitaxel is promising for further clinical use.
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Alkandari, Anfal M., Yasser M. Alsayed, and Atallah M. El-Hanbaly. "Enhanced Efficacy of Radiopharmaceuticals When Using Technetium-99m-Labeled Liposomal Agents: Synthesis and Pharmacokinetic Properties." Biomedicines 10, no. 11 (November 21, 2022): 2994. http://dx.doi.org/10.3390/biomedicines10112994.
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Challenges posed by the retention of radiopharmaceuticals in unintended organs affect the quality of patient procedures when undergoing diagnostics and therapeutics. The aim of this study was to formulate a suitable tracer encapsulated in liposomes using different techniques and compounds to enhance the stability, uptake, clearance, and cytotoxic effect of the radiopharmaceutical. Cationic liposomes were prepared by a thin-film method using dipalmitoyl phosphatidylcholine (DPPC) and cholesterol. Whole-body gamma camera images were acquired of intravenously injected New Zealand rabbits. Additionally, liposomes were assessed using stability, toxicity, zeta potential, and particle size tests. In the control cases, Technetium-99m (99mTc)-sestamibi exhibited the lowest heart uptake the blood pool and delayed images compared to both 99mTc-liposomal agents. Liver and spleen uptake in the control samples with 99mTc-sestamibi increased in 1-h-delayed images, unlike with 99mTc-liposomal agents, which were decreased in delayed images. The mean maximum count in the bladder for 99mTc-sestamibi loaded liposomes 1 h post-injection was 2354.6 (±2.6%) compared to 178.4 (±0.54%) for 99mTc-sestamibi without liposomes. Liposomal encapsulation reduced the cytotoxic effect of the sestamibi. 99mTc-MIBI-cationic liposomes exhibited excellent early uptake and clearance compared to 99mTc-MIBI without liposomes. Adding cholesterol during liposome formation enhanced the stability and specificity of the targeted organs.
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Harokopakis, Evlambia, George Hajishengallis, and Suzanne M. Michalek. "Effectiveness of Liposomes Possessing Surface-Linked Recombinant B Subunit of Cholera Toxin as an Oral Antigen Delivery System." Infection and Immunity 66, no. 9 (September 1, 1998): 4299–304. http://dx.doi.org/10.1128/iai.66.9.4299-4304.1998.
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ABSTRACT Liposomes appear to be a promising oral antigen delivery system for the development of vaccines against infectious diseases, although their uptake efficiency by Peyer’s patches in the gut and the subsequent induction of mucosal immunoglobulin A (IgA) responses remain a major concern. Aiming at targeted delivery of liposomal immunogens, we have previously reported the conjugation via a thioether bond of the GM1 ganglioside-binding subunit of cholera toxin (CTB) to the liposomal outer surface. In the present study, we have investigated the effectiveness of liposomes containing the saliva-binding region (SBR) of Streptococcus mutans AgI/II adhesin and possessing surface-linked recombinant CTB (rCTB) in generating mucosal (salivary, vaginal, and intestinal) IgA as well as serum IgG responses to the parent molecule, AgI/II. Responses in mice given a single oral dose of the rCTB-conjugated liposomes were compared to those in mice given one of the following unconjugated liposome preparations: (i) empty liposomes, (ii) liposomes containing SBR, (iii) liposomes containing SBR and coadministered with rCTB, and (iv) liposomes containing SBR plus rCTB. Three weeks after the primary immunization, significantly higher levels of mucosal IgA and serum IgG antibodies to AgI/II were observed in the rCTB-conjugated group than in mice given the unconjugated liposome preparations, although the latter mice received a booster dose at week 9. The antibody responses in mice immunized with rCTB-conjugated liposomes persisted at high levels for at least 6 months, at which time (week 26) a recall immunization significantly augmented the responses. In general, mice given unconjugated liposome preparations required one or two booster immunizations to develop a substantial anti-AgI/II antibody response, which was more prominent in the group given coencapsulated SBR and rCTB. These data indicate that conjugation of rCTB to liposomes greatly enhances their effectiveness as an antigen delivery system. This oral immunization strategy should be applicable for the development of vaccines against oral, intestinal, or sexually transmitted diseases.
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Skupin-Mrugalska, Paulina, Philipp A. Elvang, and Martin Brandl. "Application of Asymmetrical Flow Field-Flow Fractionation for Characterizing the Size and Drug Release Kinetics of Theranostic Lipid Nanovesicles." International Journal of Molecular Sciences 22, no. 19 (September 28, 2021): 10456. http://dx.doi.org/10.3390/ijms221910456.
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Liposome size and in vitro release of the active substance belong to critical quality attributes of liposomal carriers. Here, we apply asymmetric flow field-flow fractionation (AF4) to characterize theranostic liposomes prepared by thin lipid film hydration/extrusion or microfluidics. The vesicles’ size was derived from multi-angle laser light scattering following fractionation (AF4) and compared to sizes derived from dynamic light scattering measurements. Additionally, we adapted a previously developed AF4 method to study zinc phthalocyanine (ZnPc) release/transfer from theranostic liposomes. To this end, theranostic liposomes were incubated with large acceptor liposomes serving as a sink (mimicking biological sinks) and were subsequently separated by AF4. During incubation, ZnPc was transferred from donor to acceptor fraction until reaching equilibrium. The process followed first-order kinetics with half-lives between 119.5–277.3 min, depending on the formulation. The release mechanism was postulated to represent a combination of Fickian diffusion and liposome relaxation. The rate constant of the transfer was proportional to the liposome size and inversely proportional to the ZnPc/POPC molar ratio. Our results confirm the usefulness of AF4 based method to study in vitro release/transfer of lipophilic payload, which may be useful to estimate the unwanted loss of drug from the liposomal carrier in vivo.
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Medina, Oula Peñate, Tuula Peñate Medina, Jana Humbert, Bao Qi, Wolfgang Baum, Olga Will, Timo Damm, and Claus Glüer. "Using Alendronic Acid Coupled Fluorescently Labelled SM Liposomes as a Vehicle for Bone Targeting." Current Pharmaceutical Design 26, no. 46 (December 30, 2020): 6021–27. http://dx.doi.org/10.2174/1381612826666200614175905.
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Background: We recently developed a liposomal nanoparticle system that can be used for drug delivery and simultaneously be monitored by optical or photoacoustic imaging devices. Here we tested the efficacy of alendronate as a homing molecule in SM-liposomes for bone targeting. Methods: Alendronate was immobilized covalently on the liposomal surface and the fluorescent dye indocyanine green was used as a payload in the liposomes. The indocyanine green delivery was analyzed by 3D optical tomography, optical fluorescence scanner, photoacoustic imaging, and by ex-vivo biodistribution studies. Results: The results show that the alendronate, coupled to the liposomal surface, increases sphingomyelin containing liposome targeting up to several-folds. Conclusion: The alendronate targeted liposomes open possibilities for an application in active bone targeting.
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Nijen Twilhaar, Maarten K., Lucas Czentner, Joanna Grabowska, Alsya J. Affandi, Chun Yin Jerry Lau, Katarzyna Olesek, Hakan Kalay, et al. "Optimization of Liposomes for Antigen Targeting to Splenic CD169+ Macrophages." Pharmaceutics 12, no. 12 (November 25, 2020): 1138. http://dx.doi.org/10.3390/pharmaceutics12121138.
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Despite promising progress in cancer vaccination, therapeutic effectiveness is often insufficient. Cancer vaccine effectiveness could be enhanced by targeting vaccine antigens to antigen-presenting cells, thereby increasing T-cell activation. CD169-expressing splenic macrophages efficiently capture particulate antigens from the blood and transfer these antigens to dendritic cells for the activation of CD8+ T cells. In this study, we incorporated a physiological ligand for CD169, the ganglioside GM3, into liposomes to enhance liposome uptake by CD169+ macrophages. We assessed how variation in the amount of GM3, surface-attached PEG and liposomal size affected the binding to, and uptake by, CD169+ macrophages in vitro and in vivo. As a proof of concept, we prepared GM3-targeted liposomes containing a long synthetic ovalbumin peptide and tested the capacity of these liposomes to induce CD8+ and CD4+ T-cell responses compared to control liposomes or soluble peptide. The data indicate that the delivery of liposomes to splenic CD169+ macrophages can be optimized by the selection of liposomal constituents and liposomal size. Moreover, optimized GM3-mediated liposomal targeting to CD169+ macrophages induces potent immune responses and therefore presents as an interesting delivery strategy for cancer vaccination.
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Mishra, Harshita, Vaishali Chauhan, Kapil Kumar, and Deepak Teotia. "A comprehensive review on Liposomes: a novel drug delivery system." Journal of Drug Delivery and Therapeutics 8, no. 6 (November 25, 2018): 400–404. http://dx.doi.org/10.22270/jddt.v8i6.2071.
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Liposome was derived from two Greek words “Lipos meaning fat and Soma meaning body”. Liposome were spherical shaped vesicles consist of phospholipids and cholesterol. Due to their size hydrophobic and lipophilic character they are very promising system for drug delivery. This novel drug delivery system aims to target the drug directly to the site of action. Liposomes are very biocompatible and stable and have unique property to entrap both hydrophilic drug and lipophilic drug (amphiphatic nature) to its compartment and lead to controlled release effect. They are of 0.05- 5.0 micrometer in diameter. Liposomes are used for the treatment of various diseases like tumors or cancer. This article provides an overview of Liposomal Drug Delivery System and various aspects related to liposome that can be studied.
Keywords: Liposomes, novel delivery, amphiphatic, controlled release.
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Gilbreath, M. J., D. L. Hoover, C. R. Alving, G. M. Swartz, and M. S. Meltzer. "Inhibition of lymphokine-induced macrophage microbicidal activity against Leishmania major by liposomes: characterization of the physicochemical requirements for liposome inhibition." Journal of Immunology 137, no. 5 (September 1, 1986): 1681–87. http://dx.doi.org/10.4049/jimmunol.137.5.1681.
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Abstract Resident peritoneal macrophages from untreated mice develop potent microbicidal activity against amastigotes of Leishmania major after in vitro treatment with lymphokine (LK) from mitogen-stimulated spleen cells. LK-induced macrophage microbicidal activity was completely and selectively abrogated by treatment with phosphatidylcholine-phosphatidylserine (PC/PS) liposomes. Other macrophage effector functions (phagocytosis, tumoricidal activity) were unaffected, as was cytotoxicity by macrophages activated in vivo or by LK in vitro before liposome treatment. Activation factors in LK were not adsorbed or destroyed by liposomes. Liposome-induced inhibition was unaffected by indomethacin and was fully reversible: macrophages washed free of liposomes developed strong microbicidal activity with subsequent LK treatment. Changes in liposomal lipid composition markedly altered suppressive effects, but inhibition was not dependent on liposome size, cholesterol content, charge, or number of lamellae. Liposomes composed of PC alone or in combination with any of five different phospholipids were not suppressive. In contrast, inhibition was directly dependent on PS concentration within PC/PS liposomes. Phosphoserine was not inhibitory nor was dimyristoyl PS (synthetic saturated PS). However, the lysophospholipid metabolite of PS, lysoPS, was strongly suppressive. These studies suggest that the reversible and selective inhibition of LK-induced macrophage microbicidal activity by PC/PS liposomes is mediated by PS and its lysoPS metabolite.
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Tansi, Felista L., Ronny Rüger, Ansgar M. Kollmeier, Markus Rabenhold, Frank Steiniger, Roland E. Kontermann, Ulf K. Teichgräber, Alfred Fahr, and Ingrid Hilger. "Targeting the Tumor Microenvironment with Fluorescence-Activatable Bispecific Endoglin/Fibroblast Activation Protein Targeting Liposomes." Pharmaceutics 12, no. 4 (April 17, 2020): 370. http://dx.doi.org/10.3390/pharmaceutics12040370.
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Liposomes are biocompatible nanocarriers with promising features for targeted delivery of contrast agents and drugs into the tumor microenvironment, for imaging and therapy purposes. Liposome-based simultaneous targeting of tumor associated fibroblast and the vasculature is promising, but the heterogeneity of tumors entails a thorough validation of suitable markers for targeted delivery. Thus, we elucidated the potential of bispecific liposomes targeting the fibroblast activation protein (FAP) on tumor stromal fibroblasts, together with endoglin which is overexpressed on tumor neovascular cells and some neoplastic cells. Fluorescence-quenched liposomes were prepared by hydrating a lipid film with a high concentration of the self-quenching near-infrared fluorescent dye, DY-676-COOH, to enable fluorescence detection exclusively upon liposomal degradation and subsequent activation. A non-quenched green fluorescent phospholipid was embedded in the liposomal surface to fluorescence-track intact liposomes. FAP- and murine endoglin-specific single chain antibody fragments were coupled to the liposomal surface, and the liposomal potentials validated in tumor cells and mice models. The bispecific liposomes revealed strong fluorescence quenching, activatability, and selectivity for target cells and delivered the encapsulated dye selectively into tumor vessels and tumor associated fibroblasts in xenografted mice models and enabled their fluorescence imaging. Furthermore, detection of swollen lymph nodes during intra-operative simulations was possible. Thus, the bispecific liposomes have potentials for targeted delivery into the tumor microenvironment and for image-guided surgery.
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Xiao, Dexuan, and Ronghui Zhou. "Advances in the Application of Liposomal Nanosystems in Anticancer Therapy." Current Stem Cell Research & Therapy 16, no. 1 (December 1, 2021): 14–22. http://dx.doi.org/10.2174/1574888x15666200423093906.
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Cancer is the disease with the highest mortality rate, which poses a great threat to people’s lives. Cancer caused approximately 3.4 million death worldwide annually. Surgery, chemotherapy and radiotherapy are the main therapeutic methods in clinical practice. However, surgery is only suitable for patients with early-stage cancers, and chemotherapy as well as radiotherapy have various side effects, both of which limit the application of available therapeutic methods. In 1965, liposome was firstly developed to form new drug delivery systems given the unique properties of nanoparticles, such as enhanced permeability and retention effect. During the last 5 decades, liposome has been widely used for the purpose of anticancer drug delivery, and several advances have been made regarding liposomal technology, including long-circulating liposomes, active targeting liposomes and triggered release liposomes, while problems exist all along. This review introduced the advances as well as the problems during the development of liposomal nanosystems for cancer therapy in recent years.
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Sivathanu, Dr S. Bhagavathy, Shivapriya G, and Shivapriya G. "Formulation, Characterization and In vitro Drug Delivery of Vitexin Loaded Liposomes." International Journal of Pharmaceutical Sciences and Nanotechnology 14, no. 2 (April 30, 2021): 5364–71. http://dx.doi.org/10.37285/ijpsn.2021.14.2.2.
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Liposome is a spherical vesicle which contains atleast one lipid bilayer. Liposomes are used as a novel drug carriers because of its hydrophobic and hydrophilic nature, it has many advantages in the field of medical sciences. There are some other drug carriers like dendrimers, micelles, niosomes. Out of all, liposomes are considered to be the most promising agent for drug delivery. The uniqueness of liposome is when it is used as a pharmaceutical drug, it acts as a natural receptor. Thus it acts as an antigen and binds with the antibody (cancer cell) without causing any damage to the adjacent cells. For the synthesis of liposomes, a phospholipid is required. The liposomes can be synthesized using egg yolk and chloroform. So the basic phospholipid is obtained from egg yolk. For more stability, the liposomes are prepared using popc. The present work discuss about the effective preparation of drug loaded liposomes using popc (1- palmitoyl-2-oleoyl-sn-glycero-3- phosphocholine). POPC is an important phospholipid for biophysical experiments. Additionally chloroform is used as the solvent for the liposome preparation. The drug chosen for liposome loading is vitexin (vxn), which is an effective therapeutic agent against inflammation and cancer. The vesicular size, shape, drug entrapment efficacy, stability, electrochemical property and drug releasing property of the formulated liposomes were characterized. The results showed that the formulated liposomes are considered as the better drug carrier system and good choice for biotransformation within the cell to reach the target site such as cancer cells. Even though available treatments like chemotherapy and radiation therapy, causes damage to the surrounding cells, the alternative drug transferring system such as liposomal mediated drug transfer within the cell is considered as good choice of treatment to avoid such complications. The aim of liposome mediated drug carrier system is to develop a method to reach the drug to the target site. After drug delivery at the target site, the liposomes are fused within the surface of the body. This is because of the pH of liposomes, which is at 7.4 and temperature is maintained at 37 oC. So, the vxn loaded liposomes are considered as the novel drug carriers for the successful targetted drug delivery.
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Jovanović, Aleksandra A., Bojana Balanč, Mina Volić, Ilinka Pećinar, Jelena Živković, and Katarina P. Šavikin. "Rosehip Extract-Loaded Liposomes for Potential Skin Application: Physicochemical Properties of Non- and UV-Irradiated Liposomes." Plants 12, no. 17 (August 25, 2023): 3063. http://dx.doi.org/10.3390/plants12173063.
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In the present study, rosehip (Rosa canina L.) extract was successfully encapsulated in phospholipid liposomes using a single-step procedure named the proliposome method. Part of the obtained liposomes was subjected to UV irradiation and non-treated (native) and UV-irradiated liposomes were further characterized in terms of encapsulation efficiency, chemical composition (HPLC analysis), antioxidant capacity, particle size, PDI, zeta potential, conductivity, mobility, and antioxidant capacity. Raman spectroscopy as well as DSC analysis were applied to evaluate the influence of UV irradiation on the physicochemical properties of liposomes. The encapsulation efficiency of extract-loaded liposomes was higher than 90%; the average size was 251.5 nm; the zeta potential was −22.4 mV; and the conductivity was found to be 0.007 mS/cm. UV irradiation did not cause a change in the mentioned parameters. In addition, irradiation did not affect the antioxidant potential of the liposome–extract system. Raman spectroscopy indicated that the extract was completely covered by the lipid membrane during liposome entrapment, and the peroxidation process was minimized by the presence of rosehip extract in liposomes. These results may guide the potential application of rosehip extract-loaded liposomes in the food, pharmaceutical, or cosmetic industries, particularly when liposomal sterilization is needed.
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Acharya, Basanta, and Viktor Chikan. "Pulse Magnetic Fields Induced Drug Release from Gold Coated Magnetic Nanoparticle Decorated Liposomes." Magnetochemistry 6, no. 4 (October 19, 2020): 52. http://dx.doi.org/10.3390/magnetochemistry6040052.
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Magnetic nanoparticle-assisted drug release from liposomes is an important way to enhance the functionality/usefulness of liposomes. This work demonstrates an approach how to integrate magnetic nanoparticles with liposomes with the assistance of gold–thiol chemistry. The gold coated magnetic particles cover the thiolated liposomes from the outside, which removes the competition of the drug molecules and the triggering magnetic particles to free the inner space of the liposomes when compared to previous magneto liposome formulations. The liposome consists of dipalmitoyl phosphatidylcholine (DPPC) combined with distearoylphosphatidylcholine (DSPC) in addition to regular cholesterol or cholesterol-PEG-SH. Permeability assays and electron microscopy images show efficient coupling between the liposomes and nanoparticles in the presence of thiol groups without compromising the functionality of the liposomes. The nanoparticles such as gold nanoparticles, gold coated iron oxide nanoparticles and bare iron oxide nanoparticles are added following the model drug encapsulation. The efficient coupling between the gold coated nanoparticles (NPs) and the thiolate liposomes is evidenced by the shift in transition temperature of the thiolated liposomes. The addition of magnetically triggerable nanoparticles externally makes the entire interior of liposomes available for drug loading. The drug release efficiencies of these liposomes/NPs complexes were compared under exposure to pulsed magnetic fields. The results indicate up to 20% of the drug can be released in short time, which is comparable in efficiency to previous studies performed when magnetic NPs were located inside liposomes. Interestingly, the liposomes were found to exhibit variations in release efficiency based on different dilution media which is attributed to an osmotic pressure effect on liposomal stability.
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Maiti, Kuntal, Subhas Bhowmick, Pankaj Jain, Murlidhar Zope, Keyur Doshi, and Thennati Rajamannar. "Comparison of Physicochemical Properties of Generic Doxorubicin HCl Liposome Injection with the Reference Listed Drug." Anti-Cancer Agents in Medicinal Chemistry 18, no. 4 (July 17, 2018): 597–609. http://dx.doi.org/10.2174/1871520617666171121124610.
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Background: Liposomal doxorubicin is widely used for treating ovarian cancer and Kaposi’s sarcoma. Encapsulation of doxorubicin in highly complex polyethylene glycol–coated (stealth) liposomes prolongs residence time and avoids the systemic toxicity associated with administration of the free drug. Small variations in physicochemical properties introduced during manufacture of liposomes can influence the payload of encapsulated drug, stability of liposomes under physiological conditions, and release of drug at the target tissue. Accordingly, the US Food and Drug Administration and the European Medicines Agency have issued guidance for manufacturers of generic liposomal doxorubicin that is designed to ensure that more than 30 physicochemical parameters that influence its safety and efficacy should be similar in the generic and reference listed drugs. Objective: This study aims to describe the physicochemical characterization procedures used to ensure consistency between batches of generic liposomal doxorubicin and with the reference listed drug. Methods: A range of spectroscopic, chromatographic, and other physicochemical tests was used to compare relative concentrations of liposome components, liposome morphology, ratios of free/entrapped doxorubicin, stability, and in vitro doxorubicin release rates in physiologically and clinically relevant media. Results: The tests established that generic and reference liposomes contained similar concentrations of drug, lipids, and excipients and that their physical forms were also similar. Conclusion: The results of the tests demonstrate the physicochemical equivalence of generic liposomal doxorubicin hydrochloride and the reference listed drug, Doxil®/Caelyx®. Biochemical and clinical equivalence must also be demonstrated to fully meet regulatory requirements for generic liposomal medicines, and these are the subjects of separate studies.
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Damm, Dominik, Ehsan Suleiman, Hannah Theobald, Jannik T. Wagner, Mirjam Batzoni, Bianca Ahlfeld (née Kohlhauser), Bernd Walkenfort, et al. "Design and Functional Characterization of HIV-1 Envelope Protein-Coupled T Helper Liposomes." Pharmaceutics 14, no. 7 (June 30, 2022): 1385. http://dx.doi.org/10.3390/pharmaceutics14071385.
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Functionalization of experimental HIV-1 virus-like particle vaccines with heterologous T helper epitopes (T helper VLPs) can modulate the humoral immune response via intrastructural help (ISH). Current advances in the conjugation of native-like HIV-1 envelope trimers (Env) onto liposomes and encapsulation of peptide epitopes into these nanoparticles renders this GMP-scalable liposomal platform a feasible alternative to VLP-based vaccines. In this study, we designed and analyzed customizable Env-conjugated T helper liposomes. First, we passively encapsulated T helper peptides into a well-characterized liposome formulation displaying a dense array of Env trimers on the surface. We confirmed the closed pre-fusion state of the coupled Env trimers by immunogold staining with conformation-specific antibodies. These peptide-loaded Env-liposome conjugates efficiently activated Env-specific B cells, which further induced proliferation of CD4+ T cells by presentation of liposome-derived peptides on MHC-II molecules. The peptide encapsulation process was then quantitatively improved by an electrostatically driven approach using an overall anionic lipid formulation. We demonstrated that peptides delivered by liposomes were presented by DCs in secondary lymphoid organs after intramuscular immunization of mice. UFO (uncleaved prefusion optimized) Env trimers were covalently coupled to peptide-loaded anionic liposomes by His-tag/NTA(Ni) interactions and EDC/Sulfo-NHS crosslinking. EM imaging revealed a moderately dense array of well-folded Env trimers on the liposomal surface. The conformation was verified by liposomal surface FACS. Furthermore, anionic Env-coupled T helper liposomes effectively induced Env-specific B cell activation and proliferation in a comparable range to T helper VLPs. Taken together, we demonstrated that T helper VLPs can be substituted with customizable and GMP-scalable liposomal nanoparticles as a perspective for future preclinical and clinical HIV vaccine applications. The functional nanoparticle characterization assays shown in this study can be applied to other systems of synthetic nanoparticles delivering antigens derived from various pathogens.
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Adhikari, Chandan. "Liposomes-The 21st Century’s Drug Delivery System: Developments in the Last Two Decade." Asian Journal of Chemistry 35, no. 12 (December 2, 2023): 2845–69. http://dx.doi.org/10.14233/ajchem.2023.30191.
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Liposomes have been thoroughly investigated and are utilized for various illnesses for the past few decades starting from its first discovery in 1961. Since then, therapeutic efficiency of liposomes is enhanced by increasing drug absorbance while fast deterioration and adverse effects are avoided or minimized. This will extend the biological halfway life. Liposomes are more attractive for usage as drug delivery carriers with all of these characteristics and versatility to modify their surface to create additional specific functionalities. In various phases of research, there are numerous new liposomal compositions that improve the therapeutic efficiency of new and old medicines used in pre-clinical and clinical studies. Current multimodal imaging advances aimed at better diagnosing and monitoring liposome therapies as diagnostic tools. Liposomes are major possibilities for medication delivery improvement. Recent researches show that the liposomes can be taken widely in cancer treatments. The primary properties of these structures include minimal toxicity, cytocompatibility, reduced clearance rates, tissue targeting and sustained drug release. Liposomes offer a variety of benefits as shown by approval of Doxil, as compared to traditional chemotherapy with free medication treatment. There are a multitude of liposomes depending on their size, lamellar number, shape and composition. Diagnostic, therapeutic, improved vaccination are covered by clinical use of these systems. Drug and gene delivery are two therapeutic aspects, where due to their unique characteristics liposomes might be beneficial. Several illnesses have been examined with respect to the participation of liposomes, with some good results. Cancer is a life-threatening disease. These structures have been examined in this respect, both in imaging and in chemotherapy. These investigations have resulted in different liposome compositions in different clinical stages. We take this great opportunity to present various surface functionalization strategies and bio-applications of liposomes developed during the last two decades covering the notable work published from 2011 to 2021 in this review. In addition, we provide opinions on the liposome industry, its commercial market and the prospective developments in the field of liposome technology. It is anticipated that this review will serve as a valuable resource, fostering interest and engagement among scientists worldwide in the field of liposome research.
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Yue, Xiuli, and Zhifei Dai. "Liposomal Nanotechnology for Cancer Theranostics." Current Medicinal Chemistry 25, no. 12 (April 19, 2018): 1397–408. http://dx.doi.org/10.2174/0929867324666170306105350.
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Liposomes are a type of biomimetic nanoparticles generated from self-assembling concentric lipid bilayer enclosing an aqueous core domain. They have been attractive nanocarriers for the delivery of many drugs (e.g. radiopharmaceuticals, chemotherapeutic agents, porphyrin) and diagnostic agents (e.g. fluorescent dyes, quantum dots, Gadolinium complex and Fe3O4) by encapsulating (or adsorbing) hydrophilic one inside the liposomal aqueous core domain (or on the bilayer membrane surface), and by entrapping hydrophobic one within the liposomal bilayer. Additionally, the liposome surface can be easily conjugated with targeting molecules. Liposomes may accumulate in cancerous tissues not only passively via enhanced permeability and retention (EPR) effect, but also actively by targeting cancer cell or angiogenic marker specifically. The multimodality imaging functionalization of liposomal therapeutic agents makes them highly attractive for individualized monitoring of the in vivo cancer targeting and pharmacokinetics of liposomes loading therapeutic drugs, and predicting therapeutic efficacy in combination with the helpful information from each imaging technique. The present review article will highlight some main advances of cancer theranostic liposomes with a view to activate further research in the nanomedicine community.
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Borkar, Gauri, and Satyam Chemate. "Formulation Development and Evaluation Studies of Linezolid Inhaler in the Treatment of Tuberculosis." International Journal of Pharmaceutical Sciences and Drug Research 15, no. 06 (November 30, 2023): 722–29. http://dx.doi.org/10.25004/ijpsdr.2023.150605.
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The primary objective of this study was to prepare and evaluate a linezolid inhaler. Dry powder inhaler liposomes were formulated to investigate the efficacy of pulmonary delivery of linezolid for tuberculosis. The liposomes were prepared using soya lecithin and cholesterol in different weight ratios, constant amounts of drugs, and two methods: physical dispersion and ethanol injection. The F9 formulation was characterized for physical and chemical properties such as vesicle size, shape, and zeta potential. The results of physical characterization, in-vitro testing, and stability studies indicate that liposomes containing linezolid can be used for the treatment of tuberculosis. The evaluated batch exhibited favorable physicochemical properties, with spherical liposomes having a mean size below 100 nm and high entrapment efficiency (98.8%). The prepared liposomal dry powder inhalers (DPIs) sustained drug release for up to 8 hours. Liposome stability was assessed 90 days after storage at room temperature, revealing its stability. The liposomal formulation had steady zeta potential, good entrapment efficiency, improved stability, and an extended drug release time. In conclusion, linezolid-loaded liposomal inhalers were successfully formulated.
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Boafo, George Frimpong, Kosheli Thapa Magar, Marlene Davis Ekpo, Wang Qian, Songwen Tan, and Chuanpin Chen. "The Role of Cryoprotective Agents in Liposome Stabilization and Preservation." International Journal of Molecular Sciences 23, no. 20 (October 18, 2022): 12487. http://dx.doi.org/10.3390/ijms232012487.
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To improve liposomes’ usage as drug delivery vehicles, cryoprotectants can be utilized to prevent constituent leakage and liposome instability. Cryoprotective agents (CPAs) or cryoprotectants can protect liposomes from the mechanical stress of ice by vitrifying at a specific temperature, which forms a glassy matrix. The majority of studies on cryoprotectants demonstrate that as the concentration of the cryoprotectant is increased, the liposomal stability improves, resulting in decreased aggregation. The effectiveness of CPAs in maintaining liposome stability in the aqueous state essentially depends on a complex interaction between protectants and bilayer composition. Furthermore, different types of CPAs have distinct effective mechanisms of action; therefore, the combination of several cryoprotectants may be beneficial and novel attributed to the synergistic actions of the CPAs. In this review, we discuss the use of liposomes as drug delivery vehicles, phospholipid–CPA interactions, their thermotropic behavior during freezing, types of CPA and their mechanism for preventing leakage of drugs from liposomes.
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Deol, P., G. K. Khuller, and K. Joshi. "Therapeutic efficacies of isoniazid and rifampin encapsulated in lung-specific stealth liposomes against Mycobacterium tuberculosis infection induced in mice." Antimicrobial Agents and Chemotherapy 41, no. 6 (June 1997): 1211–14. http://dx.doi.org/10.1128/aac.41.6.1211.
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One recent promising development in the modification of drug formulations to improve chemotherapy is the use of a liposome-mediated drug delivery system. The efficacies of isoniazid and rifampin encapsulated in lung-specific stealth liposomes were evaluated by injecting liposomal drugs and free drugs into tuberculous mice twice a week for 6 weeks. Liposome-encapsulated drugs at and below therapeutic concentrations were more effective than free drugs against tuberculosis, as evaluated on the basis of CFUs detected, organomegaly, and histopathology. Furthermore, liposomal drugs had marginal hepatotoxicities as determined from the levels of total bilirubin and hepatic enzymes in serum. The elimination of mycobacteria from the liver and spleen was also higher with liposomal drugs than with free drugs. The encapsulation of antitubercular drugs in lung-specific stealth liposomes seems to be a promising therapeutic approach for the chemotherapy of tuberculosis.
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Saito, Shoji, Ikumi Nakashima, Aiko Hasegawa, Eiichi Akahoshi, Mitsuko Ishihara-Sugano, Shigeki Yagyu, and Yozo Nakazawa. "Tumor-Tropic Liposome-Mediated Therapeutic Delivery of mRNA for T Cell Malignancies." Blood 136, Supplement 1 (November 5, 2020): 21–22. http://dx.doi.org/10.1182/blood-2020-139020.
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Introduction : Treatment options for relapsed T cell leukemia are limited, and the prognosis remains dismal. Therefore, the development of new therapies is crucial. A liposomal delivery system has been increasingly recognized as a promising strategy for delivering both reagents and nucleic acids. However, little is known about whether the liposomal delivery of mRNA could be employed for cancer treatment. Herein, we propose a novel strategy for the treatment of T cell malignancies using tumor-tropic liposomes that can selectively deliver mRNAs of interest to leukemia cells. Methods: We tested liposomes with various lipid compositions. Leukemia cells or peripheral blood mononuclear cells (PBMCs) were cultured with rhodamine-labeled liposomes and then analyzed for rhodamine expression to investigate the selective uptake of the liposomes. To examine the selective translation of the encapsulated mRNA, the cells were incubated with liposomes loaded with firefly luciferase (ffLuc) mRNA and examined for luciferase activity. The cells were also treated with liposomes loaded with inducible caspase 9 (iC9) mRNA, with or without B/B homodimerizer (chemical-induced dimerization, CID), to examine the in vitro anti-leukemic effects. To investigate the in vivo anti-tumor effects, NSG mice were inoculated with Jurkat-ffLuc cells, and then they were intravenously treated with either liposomes loaded with iC9 or control liposomes on days 4 and 15 after tumor inoculation. Every 24, 48, and 72 h after liposome infusion, the mice were treated intraperitoneally with CID. Bioluminescence imaging was performed twice weekly to track the leukemia cell burden. Results: The screening analysis identified two types of liposomes (No. 43 and No. 79) that could selectively deliver mRNA to the cancer cells. Flow cytometry analysis showed that these liposomes labeled with rhodamine were efficiently taken up into Jurkat cells, whereas they were minimally taken up into PBMCs. Furthermore, when these two liposomes were loaded with ffLuc mRNA (43-ffLuc and 79-ffLuc), they could efficiently deliver mRNA to the cancer cells, with enhanced luciferase activity, but they minimally delivered ffLuc mRNA to PBMCs. Consistently, when these two liposomes were loaded with a suicide gene iC9 (43-iC9 and 79-iC9) in combination with CID, they effectively killed Jurkat cells and CCRF-CEM cells but minimally killed PBMCs in vitro. Furthermore, in a xenograft model of Jurkat-ffLuc, the mice treated with 79-iC9 showed significantly suppressed tumor growth compared with the mice treated with control liposome in combination with CID (Figure 1). These results suggested that the tumor-tropic liposomal delivery of iC9 mRNA could be employed for the treatment of T cell leukemia. Conclusions: Tumor-tropic liposomes can selectively deliver mRNAs of interest to leukemia cells. Moreover, tumor-tropic liposomes loaded with iC9 in combination with CID showed anti-leukemic activity both in vitro and in vivo. Thus, liposomal delivery could be a promising alternative for the treatment of T cell malignancies. Disclosures Saito: Toshiba Corporation: Research Funding. Nakashima:Toshiba Corporation: Research Funding. Hasegawa:Toshiba Corporation: Research Funding. Akahoshi:Toshiba Corporation: Current Employment. Ishihara-Sugano:Toshiba Corporation: Current Employment. Yagyu:Toshiba Corporation: Research Funding. Nakazawa:Toshiba Corporation: Research Funding.
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Jiang, Yanhao, Wenpan Li, Zhiren Wang, and Jianqin Lu. "Lipid-Based Nanotechnology: Liposome." Pharmaceutics 16, no. 1 (December 26, 2023): 34. http://dx.doi.org/10.3390/pharmaceutics16010034.
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Over the past several decades, liposomes have been extensively developed and used for various clinical applications such as in pharmaceutical, cosmetic, and dietetic fields, due to its versatility, biocompatibility, and biodegradability, as well as the ability to enhance the therapeutic index of free drugs. However, some challenges remain unsolved, including liposome premature leakage, manufacturing irreproducibility, and limited translation success. This article reviews various aspects of liposomes, including its advantages, major compositions, and common preparation techniques, and discusses present U.S. FDA-approved, clinical, and preclinical liposomal nanotherapeutics for treating and preventing a variety of human diseases. In addition, we summarize the significance of and challenges in liposome-enabled nanotherapeutic development and hope it provides the fundamental knowledge and concepts about liposomes and their applications and contributions in contemporary pharmaceutical advancement.
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Xiao, Peihong, Juan Zhao, Yi Huang, Rongrong Jin, Zhonglan Tang, Ping Wang, Xu Song, Hongfei Zhu, Zibin Yang, and Nie Yu. "A Novel Long-circulating DOX Liposome: Formulation and Pharmacokinetics Studies." Pharmaceutical Nanotechnology 8, no. 5 (November 19, 2020): 391–98. http://dx.doi.org/10.2174/2211738508666200813141454.
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Background: Doxorubicin (DOX) is a leading chemotherapeutic in cancer treatment because of its high potency and broad spectrum. Liposomal doxorubicin (Doxil®) is the first FDA-approved PEG-liposomes of DOX for the treatment of over 600,000 cancer patients, and it can overcome doxorubicin-induced cardiomyopathy and other side effects and prolong life span. The addition of MPEG2000-DSPE could elevate the total cost of cancer treatment. Objective: We intended to prepare a novel DOX liposome that was prepared with inexpensive materials egg yolk lecithin and Kolliphor HS15, thus allowing it to be much cheaper for clinical application. Methods: DOX liposomes were prepared using the combination of thin-film dispersion ultrasonic method and ammonium sulfate gradient method and the factors that influenced formulation quality were optimized. After formulation, particle size, entrapment efficiency, drug loading, stability, and pharmacokinetics were determined. Results: DOX liposomes were near-spherical morphology with the average size of 90 nm and polydispersity index (PDI) of less than 0.30. The drug loading was up to 7.5%, and the entrapment efficiency was over 80%. The pharmacokinetic studies showed that free DOX could be easily removed and the blood concentration of free DOX group was significantly lower than that of DOX liposomes, which indicated that the novel DOX liposome had a certain sustainedrelease effect. Conclusion: In summary, DOX liposome is economical and easy-prepared with prolonged circulation time. Lay Summary: Doxorubicin (DOX) is a leading chemotherapeutic in cancer treatment because of its high potency and broad spectrum. Liposomal doxorubicin (Doxil®) is the first FDAapproved PEG-liposomes of DOX to treat over 600.000 cancer patients, overcoming doxorubicin- induced cardiomyopathy and other side effects and prolonging life span. The addition of MPEG2000-DSPE could elevate the total cost of cancer treatment. We intend to prepare a novel DOX liposome prepared with inexpensive materials egg yolk lecithin and Kolliphor HS15, thus allowing it to be much cheaper for clinical use. The novel DOX liposome is economical and easy-prepared with prolonged circulation time.
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Zaske, Ana-María, Delia Danila, Michael C. Queen, Eva Golunski, and Jodie L. Conyers. "Biological Atomic Force Microscopy for Imaging Gold-Labeled Liposomes on Human Coronary Artery Endothelial Cells." Journal of Pharmaceutics 2013 (February 21, 2013): 1–8. http://dx.doi.org/10.1155/2013/875906.
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Although atomic force microscopy (AFM) has been used extensively to characterize cell membrane structure and cellular processes such as endocytosis and exocytosis, the corrugated surface of the cell membrane hinders the visualization of extracellular entities, such as liposomes, that may interact with the cell. To overcome this barrier, we used 90 nm nanogold particles to label FITC liposomes and monitor their endocytosis on human coronary artery endothelial cells (HCAECs) in vitro. We were able to study the internalization process of gold-coupled liposomes on endothelial cells, by using AFM. We found that the gold-liposomes attached to the HCAEC cell membrane during the first 15–30 min of incubation, liposome cell internalization occurred from 30 to 60 min, and most of the gold-labeled liposomes had invaginated after 2 hr of incubation. Liposomal uptake took place most commonly at the periphery of the nuclear zone. Dynasore monohydrate, an inhibitor of endocytosis, obstructed the internalization of the gold-liposomes. This study showed the versatility of the AFM technique, combined with fluorescent microscopy, for investigating liposome uptake by endothelial cells. The 90 nm colloidal gold nanoparticles proved to be a noninvasive contrast agent that efficiently improves AFM imaging during the investigation of biological nanoprocesses.
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Tretiakova, Daria, Maria Kobanenko, Irina Le-Deygen, Ivan Boldyrev, Elena Kudryashova, Natalia Onishchenko, and Elena Vodovozova. "Spectroscopy Study of Albumin Interaction with Negatively Charged Liposome Membranes: Mutual Structural Effects of the Protein and the Bilayers." Membranes 12, no. 11 (October 23, 2022): 1031. http://dx.doi.org/10.3390/membranes12111031.
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Liposomes as drug carriers are usually injected into the systemic circulation where they are instantly exposed to plasma proteins. Liposome–protein interactions can affect both the stability of liposomes and the conformation of the associated protein leading to the altered biodistribution of the carrier. In this work, mutual effects of albumin and liposomal membrane in the course of the protein’s adsorption were examined in terms of quantity of bound protein, its structure, liposome membrane permeability, and changes in physicochemical characteristics of the liposomes. Fluorescence spectroscopy methods and Fourier transform infrared spectroscopy (ATR-FTIR), which provides information about specific groups in lipids involved in interaction with the protein, were used to monitor adsorption of albumin with liposomes based on egg phosphatidylcholine with various additives of negatively charged lipidic components, such as phosphatidylinositol, ganglioside GM1, or the acidic lipopeptide. Less than a dozen of the protein molecules were tightly bound to a liposome independently of bilayer composition, yet they had a detectable impact on the bilayer. Albumin conformational changes during adsorption were partially related to bilayer microhydrophobicity. Ganglioside GM1 showed preferable features for evading undesirable structural changes.
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Alghurabi, Hamid, Tatsuaki Tagami, Koki Ogawa, and Tetsuya Ozeki. "Preparation, Characterization, and In Vitro Evaluation of Eudragit S100-Coated Bile Salt-Containing Liposomes for Oral Colonic Delivery of Budesonide." Polymers 14, no. 13 (June 30, 2022): 2693. http://dx.doi.org/10.3390/polym14132693.
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The aim of this study was to prepare a liposomal formulation of a model drug (budesonide) for colonic delivery by incorporating a bile salt (sodium glycocholate, SGC) into liposomes followed by coating with a pH-responsive polymer (Eudragit S100, ES100). The role of the SGC is to protect the liposome from the emulsifying effect of physiological bile salts, while that of ES100 is to protect the liposomes from regions of high acidity and enzymatic activity in the stomach and small intestine. Vesicles containing SGC were prepared by two preparation methods (sonication and extrusion), and then coated by ES100 (ES100-SGC-Lip). ES100-SGC-Lip showed a high entrapment efficiency (>90%) and a narrow size distribution (particle size = 275 nm, polydispersity index <0.130). The characteristics of liposomes were highly influenced by the concentration of incorporated SGC. The lipid/polymer weight ratio, liposome charge, liposome addition, and mixing rate were critical factors for efficient and uniform coating. In vitro drug release studies in various simulated fluids indicate a pH-dependent dissolution of the coating layer, and the disintegration process of ES100-SGC-Lip was evaluated. In conclusion, the bile salt-containing ES100-coated liposomal formulation has potential for effective oral colonic drug delivery.
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Baczynska, Dagmara, Katarzyna Widerak, Maciej Ugorski, and Marek Langner. "Surface Charge and the Association of Liposomes with Colon Carcinoma Cells." Zeitschrift für Naturforschung C 56, no. 9-10 (October 1, 2001): 872–77. http://dx.doi.org/10.1515/znc-2001-9-1032.
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Abstract Interaction between the plasma membrane and aggregate lipid surface determines how efficiently the encapsulated drug will be delivered into the cell. Electrostatic interactions are one of the main forces affecting liposome and aggregate association with the charged cell surface. In this study, the effect of surface charge on the association of liposomes with human colon CX-1.1 cancer cells was studied. When phosphatidylserine was incorporated into a lipid bilayer, the amount of liposomes associated with cells tended to increase along with the amount of negatively charged lipid present in the liposomal lipid bilayer. When the cationic lipid dioleoyl-1,2-diacyl-3-trimethylammonium-propane (DOTAP) was included into the liposome formula, their uptake by the cells was also increased. Maximum binding occurred when the amount of positively charged lipids in liposomes was about 10 mol% of lipids.
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Penabaka, Venugopalaiah, Chandrika Jorepalli, Harika Kandala, Nichitha Lakku, Nikhil Orugunta, Thulasi Thandra, and Prapurna Chandra Yadala. "Fabrication and characterization of hydroquinone in liposomal gel for transdermal drug delivery." Future Journal of Pharmaceuticals and Health Sciences 4, no. 3 (July 8, 2024): 29–36. http://dx.doi.org/10.26452/fjphs.v4i3.628.
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This study aimed to formulate a gel for hydroquinone dermal therapy using liposomes to maintain the active agents' concentration in the skin's deepest layers. Cholesterol was incorporated to enhance the liposome's bilayer characteristics, increasing microviscosity, membrane stability, and blister rigidity. Various methods for liposome preparation exist, but the film hydration method, being the most common, was utilized here. Results for formulation HL6, which had lower levels of Lecithin Cholesterol and rotation speed, revealed a vesicle size of 180.4 nm, a Zeta potential of -37.5 mV, and an entrapment efficiency of 69.10±1.52%. In-vitro drug release data for formulations F1, F2, and F3 within 30 minutes showed hydroquinone release rates of 97.75±0.28%, 98.92±0.56%, and 94.45±0.36%, respectively. The order of drug release was F2 > F1 > F3, with F2 demonstrating the maximum release rate. The study concludes that liposomal gel is an effective transdermal drug delivery system for therapeutic molecules. Lipid vesicles, such as liposomes, are among the best mechanisms for delivering medications to their intended locations while minimizing their dissemination to non-target tissues. This liposomal gel-based formulation shows significant potential for effectively treating acne by maintaining high concentrations of active agents in the skin's deepest layers and ensuring a controlled and sustained drug release.
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Roberts, Steven A., Chaebin Lee, Shrishti Singh, and Nitin Agrawal. "Versatile Encapsulation and Synthesis of Potent Liposomes by Thermal Equilibration." Membranes 12, no. 3 (March 11, 2022): 319. http://dx.doi.org/10.3390/membranes12030319.
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The wide-scale use of liposomal delivery systems is challenged by difficulties in obtaining potent liposomal suspensions. Passive and active loading strategies have been proposed to formulate drug encapsulated liposomes but are limited by low efficiencies (passive) or high drug specificities (active). Here, we present an efficient and universal loading strategy for synthesizing therapeutic liposomes. Integrating a thermal equilibration technique with our unique liposome synthesis approach, co-loaded targeting nanovesicles can be engineered in a scalable manner with potencies 200-fold higher than typical passive encapsulation techniques. We demonstrate this capability through simultaneous co-loading of hydrophilic and hydrophobic small molecules and targeted delivery of liposomal Doxorubicin to metastatic breast cancer cell line MDA-MB-231. Molecular dynamic simulations are used to explain interactions between Doxorubicin and liposome membrane during thermal equilibration. By addressing the existing challenges, we have developed an unparalleled approach that will facilitate the formulation of novel theranostic and pharmaceutical strategies.
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Sanarova, E. V., Zhang Xi, M. V. Dmitrieva, A. V. Lantsova, O. L. Orlova, A. P. Polozkova, N. A. Oborotova, and I. I. Krasnyuk. "FEATURES OF THE TECHNOLOGY OF LIPOSOMAL FORMULATION OF A ANALOGUE HYPOTHALAMIC HORMONE SOMATOSTATIN." Russian Journal of Biotherapy 15, no. 4 (December 30, 2016): 78–84. http://dx.doi.org/10.17650/1726-9784-2016-15-4-78-84.
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Background. In connection with the prospect of the use of an analog of the hypothalamic hormone somatostatin synthesized by the laboratory of chemical synthesis Institute of experimental diagnostics and chemotherapy of FSBI «N.N. Blokhin Russian Cancer Research Center» and showed a high anti-tumor activity as a drug arises a need to establish an optimal technology of its receipt. In preliminary studies in a modelformulation for an analog of the hypothalamic hormone somatostatin selected liposome technological process of which has a series of specific steps comprising. Objective. Development of technology for obtaining liposomal formulation hypothalamic hormone somatostatin analogue. Materials and methods. Liposomes analog of the hypothalamic hormone somatostatin obtained by method Bengema in modification for hydrophobic substances. To reduce the diameter of the liposome are used methods extrusion, homogenization and ultrasonic. Analysis of the size of the liposomes was performed by correlation spectroscopy light scattering using nanosizer. The pH of the liposomal dispersion was determined by potentiometry. The quantitative content of the drug substance was determined by spectrophotometry using a standard sample with X (282 ± 3) nm and an alcoholic solution of empty liposomes as a reference solution. Amount of incorporated drug was calculated as the ratio of the concentration of drug in the liposome dispersion after filtration to the concentration of drug in the dispersion after preparation. Results and Conclusion. The hydrophobic nature of the substance causes an analog of the hypothalamic hormone somatostatin technological features of obtaining liposomal formulation. Since the step of forming a film of the lipid substance is dissolved in an organic solvent together with lipids, film is hydrated by a solution of cryoprotectant. Grinding liposomes an analog of the hypothalamic hormone somatostatin appropriate to be carried out using homogenization or extrusion methods, due to the high efficiency of these methods, the preservation stability of the liposomes and a high percentage of inclusion an analog of the hypothalamic hormone somatostatin, included in the liposomal bilayer. At the stage of separating the non-inclusion of substance an analog of the hypothalamic hormone somatostatin due to the insolubility of the substance in the water, you can use the filtering method, without the need for complicated procedures gel filtration, dialysis, etc. Furthermore the process of separating a substance not included can be combined with the sterilization of the liposome dispersion by selecting a particular filter material.