Journal articles: 'Lipophilic drug'

1

Gulati, Monica, Manish Grover, Saranjit Singh, and Mandip Singh. "Lipophilic drug derivatives in liposomes." International Journal of Pharmaceutics 165, no. 2 (May 1998): 129–68. http://dx.doi.org/10.1016/s0378-5173(98)00006-4.

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Esteves-Pedro, Natalia Mencacci, Kenji Sugibayashi, Elissa A. Ostrosky, Marcio Ferrari, Bianca da Silva Sufi, Monica Beatriz Mathor, Paulo Roberto H. Moreno, et al. "Validation Cytotoxicity Assay for Lipophilic Substances." Current Topics in Medicinal Chemistry 18, no. 4 (May 29, 2018): 275–86. http://dx.doi.org/10.2174/1568026618666180410142829.

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It is challenging to disperse lipophilic substances in a validated cytotoxicity assay, especially for compounds with log Kow greater than or equal to 5 that may show false negative results. The purpose of this study was to explain the challenges in conducting a cytotoxicity validated test of lipophilic substances: Minthostachys setosa, Pimenta pseudocaryophyllus, and Drimysbrasiliensis essential oils. Additionally, we compared the equivalence of Neutral Red (NR) and 3- (4,5-dimethylthiazol-2-yl) -5- (3- carboxymethoxyphenyl) -2- (4-sulfophenyl) -2H -tetrazolium, inner salt (MTS) in detecting cell viability. The Hydrophile-Lipophile Balance (HLB) technique was used to evaluate the dispersion of essential oils and cytotoxicity in accordance to the guidelines of the OECD / GD 129 validated cytotoxicity assay. We compared the equivalence of vital dyes by TOST equivalence test. According to the results, we demonstrated the possibility of using other ways to disperse the lipophilic substances. Based on the HLB theory, we selected polysorbate 20 as the best solubilizing agent of the essential oils studied in D10 culture medium.

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Peixoto, F. S., P. M. Dias, G. A. Ramaldes, J. M. C. Vilela, M. S. Andrade, and A. S. Cunha. "Atomic Force Microscopy Applied to the Characterization of Solid Lipid Nanoparticles." Microscopy and Microanalysis 11, S03 (December 2005): 52–55. http://dx.doi.org/10.1017/s1431927605050877.

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Solid lipid nanoparticles (SLN) have generated increasing attention as an alternative carrier system, particularly for lipophilic drugs [1-2]. The system consists of lipid nanoparticles, which are solid at room temperature. The solid matrix offers the possibility to improve the stability against coalescence and the reduced mobility of incorporated drug molecules is a pre requisite for controlled drug release [3]. Dexamethasone acetate was used as a model drug because of its wide application in the pharmaceutical field and lipophilic properties.

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Kayipmaz, Afsin Emre, Betul Gulalp, and Sibel Benli. "Current Aspects in Lipophilic Drug Toxicity." Journal of Academic Emergency Medicine 10, no. 2 (June 1, 2011): 80–85. http://dx.doi.org/10.5152/jaem.2011.019.

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Arun Kumar, Kapil Kumar, Aparna Joshi, Ikram, and Deepak Teotia. "A Comprehensive review on Niosome: a prominent carrier in advance drug delivery." GSC Biological and Pharmaceutical Sciences 18, no. 1 (January 30, 2022): 093–99. http://dx.doi.org/10.30574/gscbps.2022.18.1.0033.

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Niosomes are vesicular nacarriers that can be used for both amphiphilic and lipophilic drugs. Niosomes are budding vehicles in advanced drug delivery systems. Niosomes are nionic surfactants vesicles that can be formed with or without the addition of cholesterol. Niosomes can be the best choice for nacarriers because of their specific characters like biodegradability, biocompatibility, and immugenic nature. Niosomes can easily trap the hydrophilic and lipophilic drugs and extend the period of the drug in the systemic circulation. Niosomes are the nacarrier that can enhance penetration of drugs into the specific target tissues hence resulting in reduced toxicity. The main aim of this review article is to provide a detailed description of Niosomes.

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Zielińska, Aleksandra, Amanda Cano, Tatiana Andreani, Carlos Martins-Gomes, Amélia M. Silva, Marlena Szalata, Ryszard Słomski, and Eliana B. Souto. "Lipid-Drug Conjugates and Nanoparticles for the Cutaneous Delivery of Cannabidiol." International Journal of Molecular Sciences 23, no. 11 (May 31, 2022): 6165. http://dx.doi.org/10.3390/ijms23116165.

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Lipid nanoparticles are currently used to deliver drugs to specific sites in the body, known as targeted therapy. Conjugates of lipids and drugs to produce drug-enriched phospholipid micelles have been proposed to increase the lipophilic character of drugs to overcome biological barriers. However, their applicability at the topical level is still minimal. Phospholipid micelles are amphiphilic colloidal systems of nanometric dimensions, composed of a lipophilic nucleus and a hydrophilic outer surface. They are currently used successfully as pharmaceutical vehicles for poorly water-soluble drugs. These micelles have high in vitro and in vivo stability and high biocompatibility. This review discusses the use of lipid-drug conjugates as biocompatible carriers for cutaneous application. This work provides a metadata analysis of publications concerning the conjugation of cannabidiol with lipids as a suitable approach and as a new delivery system for this drug.

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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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Suresh Babu P, Marina Amarendra, Subha V J, and Senthamarai S. "An analytical assessment on Mucoadhesive Buccal Drug Delivery System for improving patient convenience and compliance." International Journal of Research in Pharmaceutical Sciences 11, SPL4 (December 20, 2020): 252–58. http://dx.doi.org/10.26452/ijrps.v11ispl4.3780.

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In recent years, the novel mucoadhesive buccal drug delivery system has been developed over the conventional and systemic dosage forms. To bypass drugs from the hepatic first-pass metabolism and it enhances the bioavailability of drug at the site of administration. Absorption of a drug through the buccal mucosa reduces the degradation. Some of the enzyme activity and pH variation in the gastrointestinal tract reduces the absorption and active drug loss. To overcome this problem, the buccal route is preferred. Polymers are used in this formulation to improve the drug release rate over an extended period, and also, the therapeutic plasma level of the drug can be rapidly achieved. Overall this narrative review explains mechanism and theories, method of preparation, factors affecting mucoadhesion, advantages and limitations, applications, components used in the formulation, characterization and evaluation methods. Since the cytoplasm and intercellular spaces are hydrophilic. Lipophilic drugs have a low solubility in this environment. However, the cell membrane is rather lipophilic; it tends to difficulty permeating the hydrophilic solute through the cell membrane because of a low partition coefficient. Therefore, the cytoplasm and intercellular spaces act as a major barrier to penetration of lipophilic compounds and the cell membrane poses as an extensive transport barrier for hydrophilic compounds. Since the oral epithelial is stratified, the permeation of solute may involve these combination routes so that the route is more predictable.

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Charman, William N. "Lipids, Lipophilic Drugs, and Oral Drug Delivery—Some Emerging Concepts." Journal of Pharmaceutical Sciences 89, no. 8 (August 2000): 967–78. http://dx.doi.org/10.1002/1520-6017(200008)89:8<967::aid-jps1>3.0.co;2-r.

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Hegde, Rahul Rama, Anurag Verma, and Amitava Ghosh. "Microemulsion: New Insights into the Ocular Drug Delivery." ISRN Pharmaceutics 2013 (June 27, 2013): 1–11. http://dx.doi.org/10.1155/2013/826798.

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Delivery of drugs into eyes using conventional drug delivery systems, such as solutions, is a considerable challenge to the treatment of ocular diseases. Drug loss from the ocular surface by lachrymal fluid secretion, lachrymal fluid-eye barriers, and blood-ocular barriers are main obstacles. A number of ophthalmic drug delivery carriers have been made to improve the bioavailability and to prolong the residence time of drugs applied topically onto the eye. The potential use of microemulsions as an ocular drug delivery carrier offers several favorable pharmaceutical and biopharmaceutical properties such as their excellent thermodynamic stability, phase transition to liquid-crystal state, very low surface tension, and small droplet size, which may result in improved ocular drug retention, extended duration of action, high ocular absorption, and permeation of loaded drugs. Further, both lipophilic and hydrophilic characteristics are present in microemulsions, so that the loaded drugs can diffuse passively as well get significantly partitioned in the variable lipophilic-hydrophilic corneal barrier. This review will provide an insight into previous studies on microemulsions for ocular delivery of drugs using various nonionic surfactants, cosurfactants, and associated irritation potential on the ocular surface. The reported in vivo experiments have shown a delayed effect of drug incorporated in microemulsion and an increase in the corneal permeation of the drug.

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P, Manikandan, and Sundara Ganapathy R. "NANOEMULSIONS FOR PROSTRATE CANCER THERAPY: AN OVERVIEW." Asian Journal of Pharmaceutical and Clinical Research 10, no. 5 (May 1, 2017): 37. http://dx.doi.org/10.22159/ajpcr.2017.v10i5.17307.

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The objective of this review is to focus the inferences of low/poor bioavailability and lack of dose proportionality for the oral delivery of drugs in prostatecancer therapy. To overcome such problems, various formulation strategies has been reported including various methods for the use of surfactants,cyclodextrins, solid dispersions, micronization, permeation enhancers, and lipids. Flutamide is an antiandrogen drug and used for the therapy of prostate cancer. The flutamide drug is having limited clinical application due to its poor water solubility and needs enhancement of its dissolution rate in simulated gastric fluids. The lipid-based formulations such as nanoemulsion have been shown to improve the solubility and oral absorption of lipophilic drugs. To conclude, this article emphasizes the various approaches of nanoemulsion based formulation for prostate cancer therapy.Keywords: Nanoemulsion, Prostate cancer, Flutamide, Antiandrogen drug, Lipophilic drugs.

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Braeckmans, Marlies, Joachim Brouwers, Danny Riethorst, Cécile Servais, Jan Tack, and Patrick Augustijns. "The Influence of Fed State Lipolysis Inhibition on the Intraluminal Behaviour and Absorption of Fenofibrate from a Lipid-Based Formulation." Pharmaceutics 14, no. 1 (January 4, 2022): 119. http://dx.doi.org/10.3390/pharmaceutics14010119.

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The bioavailability of lipophilic drugs may or may not be increased when administered with food due to increased solubilisation in fed state gastrointestinal (GI) fluids. The in vivo interplay between drug solubilisation, lipid phase digestion and drug absorption is complex and remains poorly understood. This study aimed to investigate the role of fed state GI lipolysis on the intraluminal behaviour and absorption of fenofibrate, formulated as the lipid-based formulation Fenogal. Therefore, a crossover study was performed in healthy volunteers using orlistat as lipase inhibitor. Fenofibrate concentrations were determined in the proximal jejunum and linked to simultaneously assessed systemic fenofibric acid concentrations. Inhibition of lipolysis by orlistat resulted in a faster onset of absorption in 4 out of 6 volunteers, reflected by a decrease in systemic Tmax between 20 and 140 min. In addition, the increase of undigested lipids present in the small intestine upon orlistat co-administration sustained drug solubilisation for a longer period, resulting in higher fenofibrate concentrations in the jejunum and improved absorption in 5 out of 6 volunteers (median AUC0–8h 8377 vs. 5832 μM.min). Sustaining drug solubilisation in the lipid phase may thus contribute to the absorption of lipophilic drugs. More research into the different mechanisms underlying lipophilic drug absorption from fed state media at different levels of digestion is warranted.

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13

Mosqueira, V. C. F., E. A. Leite, C. M. Barros, J. M. C. Vilela, and M. S. Andrade. "Polymeric Nanostructures for Drug Delivery: Characterization by Atomic Force Microscopy." Microscopy and Microanalysis 11, S03 (December 2005): 36–39. http://dx.doi.org/10.1017/s143192760505083x.

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Formal definitions of nanotechnological devices for drug delivery typically feature the requirements that the device itself or its essential components be man-made, and in the 1-1000 nm range in at least one dimension [1]. The known nanovectors or nanostructures can be filled with drugs for different therapies and for diagnostical aims. Targeting moieties can also be attached to their surface. Polymeric nanovectors are generally made from biodegradable polymers such as polyesters, for example, poly-e-caprolactone (PCL). The drug delivery system known as nanocapsules (NCs) can be defined as a complex nanovector that is composed by a polymeric wall surrounding an oil core, where lipophilic drugs can be encapsulated. The advantages of NCs compared to other nanovectors are the high entrapment efficiencies of lipophilic drugs, low polymer content and low inherent toxicity. On the other hand, because of its complex blend of components NCs suspension allow several forms of nanovectors to be present at the same time, such as nanospheres, liposomes and nanoemulsions [2]. These ‘contaminants’ would be present in accordance with the type of formulation and method of preparation. Atomic force microscopy (AFM) has been used as a method for imaging the surfaces of liposomes [3] and nanospheres [4] allowing information in nanoscaled dimensions. In the present work, the NCs were prepared loading two different drugs, the antifungal albaconazole (ABZ), showing a crystalline drug structure and the antimalarial halofantrine (Hf) free base, having an amorphous form. These drugs possess high lipophilic character, which favours the association of the drug with the oily core, with drug loadings above 94%. Herein we studied the behavior of ABZ-loaded and Hf-loaded NCs through the AFM technique, searching to analyze and understand possible alterations induced by the drug inclusion in these nanostructures.

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Lee, K. E., S. H. Cho, H. B. Lee, S. Y. Jeong, and S. H. Yuk. "Microencapsulation of lipid nanoparticles containing lipophilic drug." Journal of Microencapsulation 20, no. 4 (January 2003): 489–96. http://dx.doi.org/10.1080/0265204031000093032.

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15

Cave, Grant, and Martyn Harvey. "Lipid Emulsion Therapy in Lipophilic Drug Toxicity." Annals of Emergency Medicine 51, no. 4 (April 2008): 449–50. http://dx.doi.org/10.1016/j.annemergmed.2007.10.014.

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Teng, Xin Rong, Dmitry G. Shchukin, and Helmuth Möhwald. "A Novel Drug Carrier: Lipophilic Drug-Loaded Polyglutamate/Polyelectrolyte Nanocontainers." Langmuir 24, no. 2 (January 2008): 383–89. http://dx.doi.org/10.1021/la702370k.

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17

Donthi, Mahipal Reddy, Siva Ram Munnangi, Kowthavarapu Venkata Krishna, Ranendra Narayan Saha, Gautam Singhvi, and Sunil Kumar Dubey. "Nanoemulgel: A Novel Nano Carrier as a Tool for Topical Drug Delivery." Pharmaceutics 15, no. 1 (January 3, 2023): 164. http://dx.doi.org/10.3390/pharmaceutics15010164.

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Nano-emulgel is an emerging drug delivery system intended to enhance the therapeutic profile of lipophilic drugs. Lipophilic formulations have a variety of limitations, which includes poor solubility, unpredictable absorption, and low oral bioavailability. Nano-emulgel, an amalgamated preparation of different systems aims to deal with these limitations. The novel system prepared by the incorporation of nano-emulsion into gel improves stability and enables drug delivery for both immediate and controlled release. The focus on nano-emulgel has also increased due to its ability to achieve targeted delivery, ease of application, absence of gastrointestinal degradation or the first pass metabolism, and safety profile. This review focuses on the formulation components of nano-emulgel for topical drug delivery, pharmacokinetics and safety profiles.

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Rajkumar, Jampala, Radha Gv, Trideva Sastri K, and Sadhana Burada. "RECENT UPDATE ON PRONIOSOMAL GEL AS TOPICAL DRUG DELIVERY SYSTEM." Asian Journal of Pharmaceutical and Clinical Research 12, no. 1 (January 7, 2019): 54. http://dx.doi.org/10.22159/ajpcr.2018.v12i1.28558.

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An existence of transdermal delivery tool, proniosomal gel, has established to showed remarkable development for lipophilic/hydrophilic drugs over additional formulations. Newer drugs of lipophilic nature emerge poor bioavailability, irregular absorption, and pharmacokinetic changes. Therefore, this novel drug delivery system has been proved advantageous over other oral and topical delivery of drug candidates to bypass such disruption. This proniosomal gel basically is a compact semi-solid liquid crystalline (gel) composed of non-ionic surfactants easily formed on dissolving the surfactant in a minimal amount of acceptable solvent and the least amount of aqueous phase and phosphate buffer. Topical application of gel under occlusive condition during which they are converted into nisomes due to hydration by water in the skin present itself. Proniosomal gels are typically present in transparent, translucent, or white semisolid gel texture, which makes them physically stable throughout storage and transport. This review provides an important overview of the preparation, formulation, evaluation, and application of proniosome gel as a drug delivery carrier.

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Rajkumar, Jampala, Radha Gv, Trideva Sastri K, and Sadhana Burada. "RECENT UPDATE ON PRONIOSOMAL GEL AS TOPICAL DRUG DELIVERY SYSTEM." Asian Journal of Pharmaceutical and Clinical Research 12, no. 1 (January 7, 2019): 54. http://dx.doi.org/10.22159/ajpcr.2019.v12i1.28558.

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An existence of transdermal delivery tool, proniosomal gel, has established to showed remarkable development for lipophilic/hydrophilic drugs over additional formulations. Newer drugs of lipophilic nature emerge poor bioavailability, irregular absorption, and pharmacokinetic changes. Therefore, this novel drug delivery system has been proved advantageous over other oral and topical delivery of drug candidates to bypass such disruption. This proniosomal gel basically is a compact semi-solid liquid crystalline (gel) composed of non-ionic surfactants easily formed on dissolving the surfactant in a minimal amount of acceptable solvent and the least amount of aqueous phase and phosphate buffer. Topical application of gel under occlusive condition during which they are converted into nisomes due to hydration by water in the skin present itself. Proniosomal gels are typically present in transparent, translucent, or white semisolid gel texture, which makes them physically stable throughout storage and transport. This review provides an important overview of the preparation, formulation, evaluation, and application of proniosome gel as a drug delivery carrier.

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Singh, Dilpreet. "Self-nanoemulsifying Drug Delivery System: A Versatile Carrier for Lipophilic Drugs." Pharmaceutical Nanotechnology 9, no. 3 (August 13, 2021): 166–76. http://dx.doi.org/10.2174/2211738509666210422124023.

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Background: Lipid-based systems such as self-nanoemulsifying drug delivery systems (SNEDDS) have resurged the eminence of nanoemulsions and offer many useful drug delivery opportunities. In the modern drug discovery era, there is a constant increase in the number of poorly soluble new chemical entities that suffer from poor and erratic bioavailability problems. The oral route possesses some major disadvantages, such as lack of constant drug levels in plasma, firstpass metabolism, which results in poor bioavailability. To address these problems, various lipidbased therapeutic systems are available from which self-enanoemulsifying systems have the potential to increase the bioavailability of poorly soluble drugs. Methods: SNEDDS is the isotropic mixture of oils, surfactant, and co-surfactant having droplet size in the range of 100-200 nm, which spontaneously emulsifies when it contacts with aqueous media in gastrointestinal (G.I) fluid. Various preparative methods are available for SNEDDS, such as high-pressure homogenizer, microfluidization, sonication, phase inversion, and shear state methods. These methods show favorable benefits in drug delivery. Self-nanoemulsifying drug delivery system possesses some disadvantages like precipitation of drug in G.I fluid or possible drug leaving in the capsule dosage form due to incompatibility issues, which can be overcome by more advanced techniques like supersaturated SNEDDS containing a precipitation inhibitor or Solid SNEDDS. These areformulated either through spray drying or using a solid carrier. Conclusion: The lipid-based nanocarrier (SNEDDS) plays a significant role in drug delivery to overcome the poor solubility and oral bioavailability. This review highlights the elaborative aspects of the diverse advantages of SNEDDS based formulations.

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Joshi, Sameer, Roderica White, Rajnish Sahu, Vida A. Dennis, and Shree R. Singh. "Comprehensive Screening of Drug Encapsulation and Co-Encapsulation into Niosomes Produced Using a Microfluidic Device." Processes 8, no. 5 (May 2, 2020): 535. http://dx.doi.org/10.3390/pr8050535.

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Microfluidics is a very facile and fast method of particulate production. Besides, it enables the manufacturing of size tuned particulate systems. Niosomes due to structural similarities have importance as alternative drug delivery systems to liposomes. Niosomes can be encapsulated or co-encapsulated with hydrophilic and lipophilic drugs. The research presented here includes the optimization of method parameters for niosome production as well as evaluation of the efficiency of microfluidics to encapsulate and co-encapsulate the drugs. For this purpose, metformin (MET) and garcinol (GC) were the model drugs. Two different non-ionic surfactants (NIS), namely Tween-20 and Span-60 with significant difference in hydrophilic-lipophilic balance (HLB) value, were chosen to analyze their efficiency to form niosomes and encapsulate one or more drugs.

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Agubata, Chukwuma. "Self-Emulsifying Formulations: A Pharmaceutical Review." Journal of Drug Delivery and Therapeutics 10, no. 3 (May 15, 2020): 231–40. http://dx.doi.org/10.22270/jddt.v10i3.3981.

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The oral route of drug delivery is commonly utilized for administration of medicines and is particularly preferred for the treatment of many chronic diseases which require continuous ingestion over a reasonably prolonged period of time. However the oral delivery of lipophilic drugs presents a major obstacle because of their low aqueous solubility. The aqueous solubility of a drug is a crucial determinant of its dissolution rate, absorption and bioavailability. Drugs with relatively high intrinsic lipophilicity can be dissolved in appropriate mixtures of oils/lipids, surfactants, cosolvents which can rapidly form oil-in-water (o/w) fine emulsions when dispersed in aqueous phase under mild agitation or mixing. These isotropic self-emulsifying formulations or self-emulsifying drug delivery systems are effective for delivery of poorly soluble, lipophilic drugs by dispersing the drugs within fine oil droplets in emulsions and this solubilization of drugs can then improve its absorption, bioavailability and therapeutic efficacy. The present paper reviews the concept, design, formulation, characterization and applications of self-emulsifying formulations. Keywords: Self-Emulsifying Formulations, lipophilicity, emulsions

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S. Pragati, S. Kuldeep, S. Ashok, and M. Satheesh. "Solid Lipid Nanoparticles: A Promising Drug Delivery Technology." International Journal of Pharmaceutical Sciences and Nanotechnology 2, no. 2 (August 31, 2009): 509–16. http://dx.doi.org/10.37285/ijpsn.2009.2.2.3.

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One of the situations in the treatment of disease is the delivery of efficacious medication of appropriate concentration to the site of action in a controlled and continual manner. Nanoparticle represents an important particulate carrier system, developed accordingly. Nanoparticles are solid colloidal particles ranging in size from 1 to 1000 nm and composed of macromolecular material. Nanoparticles could be polymeric or lipidic (SLNs). Industry estimates suggest that approximately 40% of lipophilic drug candidates fail due to solubility and formulation stability issues, prompting significant research activity in advanced lipophile delivery technologies. Solid lipid nanoparticle technology represents a promising new approach to lipophile drug delivery. Solid lipid nanoparticles (SLNs) are important advancement in this area. The bioacceptable and biodegradable nature of SLNs makes them less toxic as compared to polymeric nanoparticles. Supplemented with small size which prolongs the circulation time in blood, feasible scale up for large scale production and absence of burst effect makes them interesting candidates for study. In this present review this new approach is discussed in terms of their preparation, advantages, characterization and special features.

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Krause, H. J., A. Schwarz, and P. Rohdewald. "Polylactic acid nanoparticles, a colloidal drug delivery system for lipophilic drugs." International Journal of Pharmaceutics 27, no. 2-3 (December 1985): 145–55. http://dx.doi.org/10.1016/0378-5173(85)90064-x.

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Ali, Asad, Vaseem Ansari, Usama Ahmad, Juber Akhtar, and Afroz Jahan. "Nanoemulsion: An Advanced Vehicle For Efficient Drug Delivery." Drug Research 67, no. 11 (July 24, 2017): 617–31. http://dx.doi.org/10.1055/s-0043-115124.

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AbstractAdvanced drug delivery system has now gained preference over the conventional drug delivery system. One such research is nanoemulsion which is famous among the researchers because of ease of formation, stability, clarity, increased absorption rate leading to increasing in bioavailability and potential to form a formulation with both lipophilic as well as the hydrophilic drug. Long lasting stability (up to years) and ability to encapsulate both lipophilic and hydrophilic drug has given this colloidal system a valuable position in drug delivery. This article contains information on components required for its fabrication, preparation methods and evaluation parameters along with its application in drug delivery and future aspects of this advanced drug delivery system.

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Rajalakshmi, G., C. K. Dhanapal, and R. Sundhararajan. "An Insight to Nanostructured Lipid Carrier System." Journal of Drug Delivery and Therapeutics 10, no. 6-s (December 15, 2020): 173–82. http://dx.doi.org/10.22270/jddt.v10i6-s.4589.

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In pharmaceutical field, many drugs are being invented to combat the existing new diseases. The winds of change in the drug scenario are blowing forcefully worldwide. The emergence of new technologies provides an unique opportunities to exploit novel approaches in drug delivery. A shift from conventional drug delivery to novel drug delivery is noticed as shift from conventional drug delivery suffers from various drawbacks, But these new mighty compounds in drug therapy solely are not sufficient to meet the today’s need. There is an urgent need for the smart technology, as the drugs available suffer from serious problems like poor solubility and poor bioavailability. Most of the drugs that are available therapeutically comes under BCS class II ie, poorly soluble and high lipophilc. To assure progress in drug therapy, the development of new drugs merely is not sufficient. Issues arising in delivery of new drugs should also be addressed. Thus there is an emergent need to improve the bioavailability of these drugs, the only remedy or boon for such drugs is the discovery of some smart technologies which can improve the bioavailability of these drugs. Nano drug delivery systems are the one such universal approach which fulfills the lacuna, which exists in conventional drug delivery systems. These Nano drug delivery systems, improves the pharmacokinetic profiles of many drugs. In 1980 K. Eric Drexler developed and popularized the concept of nanotechnology. In this review a deep insight on Nano structured lipid carriers is discussed elaborating its birth, significant qualities compared to other colloidal systems, its structure, characteristics, preparation and application are spotted. Key words: BCS class, Lipophilic, Nano technology, Nano structured lipid carrier.

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Wilkins, Christi A., Lissinda H. du Plessis, and Joe M. Viljoen. "Investigating In Vitro and Ex Vivo Properties of Artemether/Lumefantrine Double-Fixed Dose Combination Lipid Matrix Tablets Prepared by Hot Fusion." Pharmaceutics 13, no. 7 (June 22, 2021): 922. http://dx.doi.org/10.3390/pharmaceutics13070922.

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Highly lipophilic antimalarial drugs, artemether and lumefantrine, whilst an effective fixed-dose combination treatment to lower the malarial disease burden, are therapeutically hindered by low aqueous solubility and varied bioavailability. This work investigates the plausibility of directly compressed lipid matrix tablets, their role as lipid-based formulations and their future standing as drug delivery systems. Lipid matrix tablets were manufactured from solid lipid dispersions in various lipid:drug ratios employing hot fusion—the melt mixing of highly lipophilic drugs with polymer(s). Sequential biorelevant dissolution media, multiple mathematical models and ex vivo analysis utilizing porcine tissue samples were employed to assess drug release kinetics and more accurately predict in vitro performance. Directly compressed stearic acid tablets in a 0.5:1 lipid:drug ratio were deemed optimal within investigated parameters. Biorelevant media was of immense value for artemether release analysis, with formulation SA0.5C1 (Stearic Acid:double fixed dose in a 0.5:1 ratio (i.e., Stearic acid 70 mg + Lumefantrine 120 mg + Artemether 20 mg); CombiLac® as filler (q.s.); and 1% w/w magnesium stearate) yielding a higher percentage of artemether release (97.21%) than the commercially available product, Coartem® (86.12%). However, dissolution media lacked the specificity to detect lumefantrine. Nonetheless, stearic acid lipid:drug ratios governed drug release mechanisms. This work demonstrates the successful utilization of lipids as pharmaceutical excipients, particularly in the formulation of lipid matrix tablets to augment the dissolution of highly lipophilic drugs, and could thus potentially improve current malarial treatment regimens.

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Sukharev, Sergei. "Mechanosensitive Channels as Sensors for Lipophilic Drug Partitioning." Biophysical Journal 104, no. 2 (January 2013): 544a. http://dx.doi.org/10.1016/j.bpj.2012.11.3013.

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Dima, Ştefan, Cristian Dima, and Gabriela Iordăchescu. "Encapsulation of Functional Lipophilic Food and Drug Biocomponents." Food Engineering Reviews 7, no. 4 (March 4, 2015): 417–38. http://dx.doi.org/10.1007/s12393-015-9115-1.

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Kadian, Renu, and Arun Nanda. "A Comprehensive Insight on Self Emulsifying Drug Delivery Systems." Recent Advances in Drug Delivery and Formulation 16, no. 1 (April 2022): 15–43. http://dx.doi.org/10.2174/2667387815666211207112803.

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Background: The oral route is a highly recommended route for the delivery of a drug. But most lipophilic drugs are difficult to deliver via this route due to their low aqueous solubility. Selfemulsifying drug delivery systems (SEDDS) have emerged as a potential approach of increasing dissolution of a hydrophobic drug due to spontaneous dispersion in micron or nano sized globules in the GI tract under mild agitation. Objective: The main motive of this review article is to describe the mechanisms, advantages, disadvantages, factors affecting, effects of excipients, possible mechanisms of enhancing bioavailability, and evaluation of self-emulsifying drug delivery systems. Result: Self emulsifying systems incorporate the hydrophobic drug inside the oil globules, and a monolayer is formed by surfactants to provide the low interfacial tension, which leads to improvement in the dissolution rate of hydrophobic drugs. The globule size of self-emulsifying systems depends upon the type and ratio of excipients in which they are used. The ternary phase diagram is constructed to find out the range of concentration of excipients used. This review article also presents recent and updated patents on self-emulsifying drug delivery systems. Self-emulsifying systems have the ability to enhance the oral bioavailability and solubility of lipophilic drugs. Conclusion: This technique offers further advantages such as bypassing the first pass metabolism via absorption of drugs through the lymphatic system, easy manufacturing, reducing enzymatic hydrolysis, inter and intra subject variability, and food effects.

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de Almeida, Camila, Claudio Diniz, Vania Silva, Mauricio Saraiva, Mireille Le Hyaric, and Mauro de Almeida. "Antibacterial Activity of Lipophilic Fluoroquinolone Derivatives." Medicinal Chemistry 5, no. 5 (September 1, 2009): 419–21. http://dx.doi.org/10.2174/157340609789117859.

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Shah, Sharmila, Roshan Bodhe, and Ashish Gorle. "Formulation Development of Porous Mannitol carrier: Improving the dissolution of poorly soluble drugs." Journal of Drug Delivery and Therapeutics 9, no. 6 (November 15, 2019): 143–54. http://dx.doi.org/10.22270/jddt.v9i6.3719.

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Major challenges in the design of oral dosage forms are their low solubility and low bioavailability. Improving the dissolution of these oral dosage forms are one of the most challenging tasks for the formulation scientists as most of the drug candidates are highly lipophilic in nature. Telmisartan and Ezetimibe belongs to the BCS class II, having high lipophilicity, poor water solubility and poor dissolution. The objective of this work was to improve the dissolution rate of poorly water soluble drugs by using porous carrier drug delivery system. Templating based spray drying methodology was used to prepare porous mannitol. Drug (Telmisartan, Ezetimibe) loaded porous mannitol carriers then characterized by P-XRD, DSC, SEM, BET surface area analysis and ATR-FTIR. ATR-FTIR studies showed complete removal of templating agent from carrier. P-XRD and DSC studies confirmed nano- confinement of drug in crystalline form. In vitro dissolution study results indicated that porous mannitol prepared using tartaric acid as templating agent showed significant improvement in dissolution rate than pure drugs and respective physical mixtures .These results suggest that, these porous carriers can be useful as drug carriers for improving the dissolution of lipophilic drugs. Keywords: Templating agent, Spray drying, Mannitol, Surface area, Tartaric acid.

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Tay, Erin, Tri-Hung Nguyen, Leigh Ford, Hywel D. Williams, Hassan Benameur, Peter J. Scammells, and Christopher J. H. Porter. "Ionic Liquid Forms of the Antimalarial Lumefantrine in Combination with LFCS Type IIIB Lipid-Based Formulations Preferentially Increase Lipid Solubility, In Vitro Solubilization Behavior and In Vivo Exposure." Pharmaceutics 12, no. 1 (December 22, 2019): 17. http://dx.doi.org/10.3390/pharmaceutics12010017.

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Lipid based formulations (LBFs) are commonly employed to enhance the absorption of highly lipophilic, poorly water-soluble drugs. However, the utility of LBFs can be limited by low drug solubility in the formulation. Isolation of ionizable drugs as low melting, lipophilic salts or ionic liquids (ILs) provides one means to enhance drug solubility in LBFs. However, whether different ILs benefit from formulation in different LBFs is largely unknown. In the current studies, lumefantrine was isolated as a number of different lipophilic salt/ionic liquid forms and performance was assessed after formulation in a range of LBFs. The solubility of lumefantrine in LBF was enhanced 2- to 80-fold by isolation as the lumefantrine docusate IL when compared to lumefantrine free base. The increase in drug loading subsequently enhanced concentrations in the aqueous phase of model intestinal fluids during in vitro dispersion and digestion testing of the LBF. To assess in vivo performance, the systemic exposure of lumefantrine docusate after administration in Type II-MCF, IIIB-MCF, IIIB-LCF, and IV formulations was evaluated after oral administration to rats. In vivo exposure was compared to control lipid and aqueous suspension formulations of lumefantrine free base. Lumefantrine docusate in the Type IIIB-LCF showed significantly higher plasma exposure compared to all other formulations (up to 35-fold higher). The data suggest that isolation of a lipid-soluble IL, coupled with an appropriate formulation, is a viable means to increase drug dose in an oral formulation and to enhance exposure of lumefantrine in vivo.

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Wagle, Susbin Raj, Bozica Kovacevic, Daniel Walker, Corina Mihaela Ionescu, Melissa Jones, Goran Stojanovic, Sanja Kojic, Armin Mooranian, and Hani Al-Salami. "Pharmacological and Advanced Cell Respiration Effects, Enhanced by Toxic Human-Bile Nano-Pharmaceuticals of Probucol Cell-Targeting Formulations." Pharmaceutics 12, no. 8 (July 29, 2020): 708. http://dx.doi.org/10.3390/pharmaceutics12080708.

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Bile acids have recently been studied for potential applications as formulation excipients and enhancers for drug release; however, some bile acids are not suitable for this application. Unconjugated lithocholic acid (ULCA) has recently shown drug formulation-stabilizing and anti-inflammatory effects. Lipophilic drugs have poor gut absorption after an oral dose, which necessitates the administration of high doses and causes subsequent side effects. Probucol (PB) is a highly lipophilic drug with poor oral absorption that resulted in restrictions on its clinical prescribing. Hence, this study aimed to design new delivery systems for PB using ULCA-based matrices and to test drug formulation, release, temperature, and biological effects. ULCA-based matrices were formulated for PB oral delivery by applying the jet-flow microencapsulation technique using sodium alginate as a polymer. ULCA addition to new PB matrices improved the microcapsule’s stability, drug release in vitro (formulation study), and showed a promising effect in ex vivo study (p < 0.05), suggesting that ULCA can optimize the oral delivery of PB and support its potential application in diabetes treatment.

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Li, Yang, Jiao Zhu, Tianyi Kang, Yuwen Chen, Yu Liu, Yulan Huang, Yi Luo, Meijuan Huang, and Maling Gou. "Co-assembling FRET nanomedicine with self-indicating drug release." Chemical Communications 54, no. 82 (2018): 11618–21. http://dx.doi.org/10.1039/c8cc06792a.

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Khasanova, Svetlana Rashitovna, Natal'ya Vladimirovna Kudashkina, Valeriya Andreyevna Gusakova, and Nadira Begim Kursanovna Jalalova. "COMPARATIVE ANALYSIS OF THE CHEMICAL COMPOSITION OF LIPOPHILIC FRACTIONS OF SHOOTS OF THREE SPECIES OF THE GENUS CRATAEGUS L." chemistry of plant raw material, no. 4 (December 14, 2021): 373–80. http://dx.doi.org/10.14258/jcprm.2021048804.

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The article presents research of the chemical composition of lipophilic fractions of shoots Crataegus sanguinea Pall. (Rosaceae), Crataegus submollis Sarg. (Rosaceae) and Crataegus almaatensis Pojark. (Rosaceae). Lipophilic extract is obtained from petroleum ether. The components of the lipophilic fraction were separated and identified by gas chromatography with mass spectrometry. 36 compounds were identified in lipophilic fractions: hydrocarbons, fatty acids, sugars, phenolic compounds, diterpenoids and sterols. Their presence may determine the pharmacological properties of hawthorn shoots. These research expand information about the chemical composition of these hawthorn species and can be used in the development of a new drug.

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Siqueira Leite, Claudia Batista, Janaina Moreira Coelho, Luis Alexandre Muehlmann, Ricardo Bentes Azevedo, and Marcelo Henrique Sousa. "Microemulsions as Platforms for Transdermal Delivery of Hydrophilic Drugs - A Review." Current Nanoscience 14, no. 3 (April 18, 2018): 170–78. http://dx.doi.org/10.2174/1573413714666171218145416.

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Background: Delivery rates in cutaneous applications are limited by the skin barrier and also by the physical-chemical properties of the drug in the formulation. A lipophilic drug has more affinity, and can permeate the epidermis more easily than a hydrophilic drug. The potential use of nano-sized dispersions as distribution systems for hydrophilic drugs is being investigated. Objective: To analyze the literature with regard to the development of microemulsions (ME) for transdermal delivery of hydrophilic drugs, with a view to identifying strategies to increase the permeation of these drugs. Results: One hundred and eleven articles were potentially relevant to the combination of search criteria. After excluding duplicated articles, the abstracts of 83 articles were read. Of these, 73 did not meet the inclusion criteria. To complete the review process, the whole text of 10 articles was evaluated. Conclusion: The main factors that positively influenced the permeation of hydrophilic drugs were low hydrophilic-lipophilic balance (HLB) values of the surfactant; concentrations of about 40% of surfactants and 30% of aqueous phase for the water-in-oil (W/O) systems; the addition of permeation promoters to the systems; and the association of physical methods during the application of the ME. The results offered support for the development of new topical microemulsions for hydrophilic drug delivery.

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Desfrançois, Claire, Rachel Auzély, and Isabelle Texier. "Lipid Nanoparticles and Their Hydrogel Composites for Drug Delivery: A Review." Pharmaceuticals 11, no. 4 (November 1, 2018): 118. http://dx.doi.org/10.3390/ph11040118.

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Several drug delivery systems already exist for the encapsulation and subsequent release of lipophilic drugs that are well described in the scientific literature. Among these, lipid nanoparticles (LNP) have specifically come up for dermal, transdermal, mucosal, intramuscular and ocular drug administration routes in the last twenty years. However, for some of them (especially dermal, transdermal, mucosal), the LNP aqueous dispersions display unsuitable rheological properties. They therefore need to be processed as semi-solid formulations such as LNP-hydrogel composites to turn into versatile drug delivery systems able to provide precise spatial and temporal control of active ingredient release. In the present review, recent developments in the formulation of lipid nanoparticle-hydrogel composites are highlighted, including examples of successful encapsulation and release of lipophilic drugs through the skin, the eyes and by intramuscular injections. In relation to lipid nanoparticles, a specific emphasis has been put on the LNP key properties and how they influence their inclusion in the hydrogel. Polymer matrices include synthetic polymers such as poly(acrylic acid)-based materials, environment responsive (especially thermo-sensitive) polymers, and innovative polysaccharide-based hydrogels. The composite materials constitute smart, tunable drug delivery systems with a wide range of features, suitable for dermal, transdermal, and intramuscular controlled drug release.

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Chen, Feng, Li Li, and Dan-Dan Tian. "Salvia miltiorrhizaRoots against Cardiovascular Disease: Consideration of Herb-Drug Interactions." BioMed Research International 2017 (2017): 1–12. http://dx.doi.org/10.1155/2017/9868694.

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Salvia miltiorrhizaroot (Danshen) is widely used in Asia for its cardiovascular benefits and contains both hydrophilic phenolic acids and lipophilic tanshinones, which are believed to be responsible for its therapeutic efficacy. This review summarized the effects of these bioactive components fromS. miltiorrhizaroots on pharmacokinetics of comedicated drugs with mechanic insights regarding alterations of protein binding, enzyme activity, and transporter activity based on the published data stemming from bothin vitroandin vivohuman studies.In vitrostudies indicated that cytochrome P450 (CYP450), carboxylesterase enzyme, catechol-O-methyltransferase, organic anion transporter 1 (OAT1) and OAT3, and P-glycoprotein were the major targets involved inS. miltiorrhiza-drug interactions. Lipophilic tanshinones had much more potent inhibitory effects towards CYPs activities compared to hydrophilic phenolic acids, evidenced by much lowerKivalues of the former. ClinicalS. miltiorrhiza-drug interaction studies were mainly conducted using CYP1A2 and CYP3A4 probe substrates. In addition, the effects of coexisting components on the pharmacokinetic behaviors of those noted bioactive compounds were also included herein.

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Bhardwaj, Snigdha, and Ashutosh Tiwari. "Nanoemulgel: a Promising Nanolipoidal-Emulsion Based Drug Delivery System in Managing Psoriasis." Dhaka University Journal of Pharmaceutical Sciences 20, no. 2 (December 29, 2021): 235–46. http://dx.doi.org/10.3329/dujps.v20i2.57174.

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Nanomedicine, a novel concept, bears much hope in delivering drug candidates having low solubility and bioavailability. Nano-emulgel, one of the emerging tools, is considered as ideal carriers for the topical delivery of lipophilic drugs to overcome these challenges in the management of psoriasis and related skin problems. Psoriasis is an auto-immune and chronic inflammatory disease affecting 2-3% population of the world. Current available treatment of psoriasis has limitations such as systemic side effects and low percutaneous permeation, which evokes a dire need to develop an alternative lipoidal nanocarrier system. Nano-emulgel is basically formed by admixing nanoemulsion system with a hydrogel matrix using both high and low energy methods. Various literatures have been reported for lipoidal nanocarriers in topical treatment suggesting reduced dose, improved percutaneous absorption and better bioavailability of lipophilic drugs with nano-emulgel delivery via topical route. Several approved marketed preparations are available that strongly support the stability of these nanocarriers in respect to its efficacy and safety. This supports the fact of using topical nano-emulgel system to deliver lipophilic drugs to overcome the sufferings from oral delivery and improved patient compliance. Therefore, it is suggested as a potential system that can be used for an effective management of psoriasis via topical route in near future. Dhaka Univ. J. Pharm. Sci. 20(2): 235-246, 2021 (December)

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Li, Yang, Shujuan Wang, Yulan Huang, Yuwen Chen, Wenbi Wu, Yu Liu, Jing Zhang, Yue Feng, Xian Jiang, and Maling Gou. "Light-activated drug release from prodrug nanoassemblies by structure destruction." Chemical Communications 55, no. 87 (2019): 13128–31. http://dx.doi.org/10.1039/c9cc06673j.

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Sonawale, Pratiksha, Amol Patil, Asmit Kamble, and Mangesh Bhutkar. "Solubility Enhancement of Lipophilic Drugs-Solid Self Micro-Emulsifying Drug Delivery System." Asian Journal of Pharmacy and Technology 6, no. 3 (2016): 155. http://dx.doi.org/10.5958/2231-5713.2016.00022.2.

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Rivers-Auty, Jack, and John Ashton. "Vehicles for Lipophilic Drugs: Implications for Experimental Design, Neuroprotection, and Drug Discovery." Current Neurovascular Research 10, no. 4 (August 31, 2013): 356–60. http://dx.doi.org/10.2174/15672026113109990021.

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Warnakulasuriya Thanujee Fernando, Athuraliya Gamacharige Kasuni Neranja, and Samamalee Upekshi Kankanamge. "A review on various plant-derived nanoemulgels and their applications." World Journal of Advanced Research and Reviews 15, no. 3 (September 30, 2022): 214–21. http://dx.doi.org/10.30574/wjarr.2022.15.3.0916.

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Nanoemulgel is an emergent and promising drug delivery system used nowadays in the pharmaceutical industry. As a novel transdermal drug delivery tool, the applications of nanoemulgel have increasingly been used due to their unique characteristic properties and benefits over other oral and topical drug deliveries to avoid poor drug bioavailability and pharmacokinetic variations. These nanoemulgels are principally oil-in-water nanoemulsions gelled with a certain gelling agent in them. Plant extracts provide remarkable therapeutic options to manage different disease conditions due to their various pharmacological activities such as antioxidant, anti-inflammatory, anti-cancer, antibacterial, etc. However, the poor solubility and low bioavailability of lipophilic phytochemicals in plant extracts are two major issues in developing plant-derived formulations. In the past years, pharmaceutical research has focused more on nano-scale delivery systems to overcome the above problems by improving the delivery of herbal extracts and they have also reported nanoemulgel as a good vehicle for lipophilic and poorly soluble drugs. Therefore, the objective of this review is to discuss recent studies and applications of plant-derived nanoemulgels.

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Carneiro, Tatiana J., Rita Araújo, Martin Vojtek, Salomé Gonçalves-Monteiro, Ana L. M. Batista de Carvalho, Maria Paula M. Marques, Carmen Diniz, and Ana M. Gil. "Impact of the Pd2Spm (Spermine) Complex on the Metabolism of Triple-Negative Breast Cancer Tumors of a Xenograft Mouse Model." International Journal of Molecular Sciences 22, no. 19 (October 5, 2021): 10775. http://dx.doi.org/10.3390/ijms221910775.

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The interest in palladium(II) compounds as potential new anticancer drugs has increased in recent years, due to their high toxicity and acquired resistance to platinum(II)-derived agents, namely cisplatin. In fact, palladium complexes with biogenic polyamines (e.g., spermine, Pd2Spm) have been known to display favorable antineoplastic properties against distinct human breast cancer cell lines. This study describes the in vivo response of triple-negative breast cancer (TNBC) tumors to the Pd2Spm complex or to cisplatin (reference drug), compared to tumors in vehicle-treated mice. Both polar and lipophilic extracts of tumors, excised from a MDA-MB-231 cell-derived xenograft mouse model, were characterized through nuclear magnetic resonance (NMR) metabolomics. Interestingly, the results show that polar and lipophilic metabolomes clearly exhibit distinct responses for each drug, with polar metabolites showing a stronger impact of the Pd(II)-complex compared to cisplatin, whereas neither drug was observed to significantly affect tumor lipophilic metabolism. Compared to cisplatin, exposure to Pd2Spm triggered a higher number of, and more marked, variations in some amino acids, nucleotides and derivatives, membrane precursors (choline and phosphoethanolamine), dimethylamine, fumarate and guanidine acetate, a signature that may be relatable to the cytotoxicity and/or mechanism of action of the palladium complex. Putative explanatory biochemical hypotheses are advanced on the role of the new Pd2Spm complex in TNBC metabolism.

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Knoke, Sabrina, and Heike Bunjes. "Transfer Investigations of Lipophilic Drugs from Lipid Nanoemulsions to Lipophilic Acceptors: Contributing Effects of Cholesteryl Esters and Albumin as Acceptor Structures." Pharmaceuticals 14, no. 9 (August 28, 2021): 865. http://dx.doi.org/10.3390/ph14090865.

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When studying the release of poorly water-soluble drugs from colloidal drug delivery systems designed for intravenous administration, the release media should preferentially contain lipophilic components that represent the physiological acceptors present in vivo. In this study, the effect of different acceptor structures was investigated by comparing the transfer of fenofibrate, retinyl acetate, and orlistat from trimyristin nanoemulsion droplets into lipid-containing hydrogel particles, as well as to bovine serum albumin (BSA). A nanodispersion based on trimyristin and cholesteryl nonanoate was incorporated into the hydrogel particles (mean diameter ~40 µm) in order to mimic the composition of lipoproteins. The course of transfer observed utilizing the lipid-containing hydrogel particles as an acceptor was in relation to the lipophilicity of the drugs: the higher the logP value, the slower the transfer. There was no detectable amount of the drugs transferred to BSA in liquid solution, demonstrating clearly that albumin alone does not contribute substantially as acceptor for the lipophilic drugs under investigation in this study. In contrast, cholesteryl nonanoate contributes to a much greater extent. However, in all cases, the partition equilibrium of the drugs under investigation was in favor of the trimyristin emulsion droplets.

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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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Khatioda, Rajiv, Basanta Saikia, Pranab Jyoti Das, and Bipul Sarma. "Solubility and in vitro drug permeation behavior of ethenzamide cocrystals regulated in physiological pH environments." CrystEngComm 19, no. 46 (2017): 6992–7000. http://dx.doi.org/10.1039/c7ce01626c.

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Drug release behavior of few ethenzamide cocrystals was investigated at different pH buffers. Change in lipophilic behavior and conformational adjustment of drug along with supramolecular synthons were probed for their improved drug efficacy.

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Kaushik, Vasudha, Yameera Ganashalingam, Robert Schesny, Christian Raab, Soma Sengupta, and Cornelia M. Keck. "Influence of Massage and Skin Hydration on Dermal Penetration Efficacy of Nile Red from Petroleum Jelly—An Unexpected Outcome." Pharmaceutics 13, no. 12 (December 18, 2021): 2190. http://dx.doi.org/10.3390/pharmaceutics13122190.

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The study aimed at comparing the influence of direct and indirect skin hydration as well as massage on the dermal penetration efficacy of active compounds. Nile red was used as a lipophilic drug surrogate and was incorporated into Vaseline (petroleum jelly). The formulation was applied with and without massage onto either dry skin or pre-hydrated, moist skin. It was expected that the occlusive properties of Vaseline in combination with massage and enhanced skin hydration would cause a superposition of penetration-enhancing effects, which should lead to a tremendous increase in the dermal penetration efficacy of the lipophilic drug surrogate. Results obtained were diametral to the expectations, and various reasons were identified for causing the effect observed. Firstly, it was found that Vaseline undergoes syneresis after topical application. The expulsed mineral oil forms a film on top of the skin, and parts of it penetrate into the skin. The lipophilic drug surrogate, which is dissolved in the mineral oil, enters the skin with the mineral oil, i.e., via a solvent drag mechanism. Secondly, it was found that massage squeezes the skin and causes the expulsion of water from deeper layers of the SC. The expulsed water can act as a water barrier that prevents the penetration of lipophilic compounds and promotes the penetration of hydrophilic compounds. Based on the data, it is concluded that dermal penetration is a complex process that cannot only be explained by Fick’s law. It is composed of at least three different mechanisms. The first mechanism is the penetration of active ingredients with their solvents into the skin (convection, solvent drag), the second mechanism is the penetration of the active ingredient via passive diffusion, and the third mechanism can involve local penetration phenomena, e.g., the formation of liquid menisci and particle-associated penetration enhancement, which occur upon the evaporation of water and/or other ingredients from the formulation on top of the skin.

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Žabka, M., M. Hukeľová, M. Čuchorová, and L. Starýchová. "Effect of microemulsion on liberation of indomethacin from hydrophilic and lipophilic gel." Acta Facultatis Pharmaceuticae Universitatis Comenianae 59, no. 1 (January 1, 2012): 81–88. http://dx.doi.org/10.2478/v10219-012-0018-4.

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Effect of microemulsion on liberation of indomethacin from hydrophilic and lipophilic gelThe paper is focused on liberation of indomethacin from gels and the influence of microemulsion's presence in the system. Liberation of drug was performed in vitro through a semipermeable membrane and drug quantity was determined spectrophotometrically. Our results pointed out that the influence of microemulsion system on drug liberation depends on the gel selection. The presence of o/w microemulsion in the lipophilic gel (aerosil in liquid paraffin) increased the released amount of the drug approximately 50%. The liberation profile of indomethacin is better when the hydrophilic gel (carbopol) was used. Drug was released in higher amounts from hydrophilic gel comparised to the commercial gel. The presence of microemulsion in carbopol gel did not have any significant influence.

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Journal articles on the topic 'Lipophilic drug'

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