Journal articles: 'Lipid nanoparticles of nonlamellar lipids'

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Mertins, Omar, Patrick D. Mathews, and Angelina Angelova. "Advances in the Design of pH-Sensitive Cubosome Liquid Crystalline Nanocarriers for Drug Delivery Applications." Nanomaterials 10, no. 5 (May 18, 2020): 963. http://dx.doi.org/10.3390/nano10050963.

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Nanostructure bicontinuous cubic phase self-assembled materials are receiving expanding applications as biocompatible delivery systems in various therapeutic fields. The functionalization of cubosome, spongosome, hexosome and liposome nanocarriers by pH-sensitive lipids and/or pH-sensitive polymer shells offers new opportunities for oral and topical drug delivery towards a new generation of cancer therapies. The electrochemical behavior of drug compounds may favor pH-triggered drug release as well. Here, we highlight recent investigations, which explore the phase behavior of mixed nonlamellar lipid/fatty acid or phospholipid systems for the design of pH-responsive and mucoadhesive drug delivery systems with sustained-release properties. X-ray diffraction and small-angle X-ray scattering (SAXS) techniques are widely used in the development of innovative delivery assemblies through detailed structural analyses of multiple amphiphilic compositions from the lipid/co-lipid/water phase diagrams. pH-responsive nanoscale materials and nanoparticles are required for challenging therapeutic applications such as oral delivery of therapeutic proteins and peptides as well as of poorly water-soluble substances. Perspective nanomedicine developments with smart cubosome nanocarriers may exploit compositions elaborated to overcome the intestinal obstacles, dual-drug loaded pH-sensitive liquid crystalline architectures aiming at enhanced therapeutic efficacy, as well as composite (lipid/polyelectrolyte) types of mucoadhesive controlled release colloidal cubosomal formulations for the improvement of the drugs’ bioavailability.

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Nakano, Minoru. "Preparation and Structural Investigation of Lipid Nanoparticles with Nonlamellar Phases." MEMBRANE 31, no. 4 (2006): 202–6. http://dx.doi.org/10.5360/membrane.31.202.

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Zerkoune, Leïla, Sylviane Lesieur, Jean-Luc Putaux, Luc Choisnard, Annabelle Gèze, Denis Wouessidjewe, Borislav Angelov, Corinne Vebert-Nardin, James Doutch, and Angelina Angelova. "Mesoporous self-assembled nanoparticles of biotransesterified cyclodextrins and nonlamellar lipids as carriers of water-insoluble substances." Soft Matter 12, no. 36 (2016): 7539–50. http://dx.doi.org/10.1039/c6sm00661b.

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Leu, Jassica S. L., Jasy J. X. Teoh, Angel L. Q. Ling, Joey Chong, Yan Shan Loo, Intan Diana Mat Azmi, Noor Idayu Zahid, Rajendran J. C. Bose, and Thiagarajan Madheswaran. "Recent Advances in the Development of Liquid Crystalline Nanoparticles as Drug Delivery Systems." Pharmaceutics 15, no. 5 (May 6, 2023): 1421. http://dx.doi.org/10.3390/pharmaceutics15051421.

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Due to their distinctive structural features, lyotropic nonlamellar liquid crystalline nanoparticles (LCNPs), such as cubosomes and hexosomes, are considered effective drug delivery systems. Cubosomes have a lipid bilayer that makes a membrane lattice with two water channels that are intertwined. Hexosomes are inverse hexagonal phases made of an infinite number of hexagonal lattices that are tightly connected with water channels. These nanostructures are often stabilized by surfactants. The structure’s membrane has a much larger surface area than that of other lipid nanoparticles, which makes it possible to load therapeutic molecules. In addition, the composition of mesophases can be modified by pore diameters, thus influencing drug release. Much research has been conducted in recent years to improve their preparation and characterization, as well as to control drug release and improve the efficacy of loaded bioactive chemicals. This article reviews current advances in LCNP technology that permit their application, as well as design ideas for revolutionary biomedical applications. Furthermore, we have provided a summary of the application of LCNPs based on the administration routes, including the pharmacokinetic modulation property.

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Eleraky, Nermin E., Ayat Allam, Sahar B. Hassan, and Mahmoud M. Omar. "Nanomedicine Fight against Antibacterial Resistance: An Overview of the Recent Pharmaceutical Innovations." Pharmaceutics 12, no. 2 (February 8, 2020): 142. http://dx.doi.org/10.3390/pharmaceutics12020142.

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Based on the recent reports of World Health Organization, increased antibiotic resistance prevalence among bacteria represents the greatest challenge to human health. In addition, the poor solubility, stability, and side effects that lead to inefficiency of the current antibacterial therapy prompted the researchers to explore new innovative strategies to overcome such resilient microbes. Hence, novel antibiotic delivery systems are in high demand. Nanotechnology has attracted considerable interest due to their favored physicochemical properties, drug targeting efficiency, enhanced uptake, and biodistribution. The present review focuses on the recent applications of organic (liposomes, lipid-based nanoparticles, polymeric micelles, and polymeric nanoparticles), and inorganic (silver, silica, magnetic, zinc oxide (ZnO), cobalt, selenium, and cadmium) nanosystems in the domain of antibacterial delivery. We provide a concise description of the characteristics of each system that render it suitable as an antibacterial delivery agent. We also highlight the recent promising innovations used to overcome antibacterial resistance, including the use of lipid polymer nanoparticles, nonlamellar liquid crystalline nanoparticles, anti-microbial oligonucleotides, smart responsive materials, cationic peptides, and natural compounds. We further discuss the applications of antimicrobial photodynamic therapy, combination drug therapy, nano antibiotic strategy, and phage therapy, and their impact on evading antibacterial resistance. Finally, we report on the formulations that made their way towards clinical application.

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Nguyễn, Cảnh Hưng, Jean-Luc Putaux, Gianluca Santoni, Sana Tfaili, Sophie Fourmentin, Jean-Baptiste Coty, Luc Choisnard, et al. "New nanoparticles obtained by co-assembly of amphiphilic cyclodextrins and nonlamellar single-chain lipids: Preparation and characterization." International Journal of Pharmaceutics 531, no. 2 (October 2017): 444–56. http://dx.doi.org/10.1016/j.ijpharm.2017.07.007.

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Vandoolaeghe, Pauline, Justas Barauskas, Markus Johnsson, Fredrik Tiberg, and Tommy Nylander. "Interaction between Lamellar (Vesicles) and Nonlamellar Lipid Liquid-Crystalline Nanoparticles as Studied by Time-Resolved Small-Angle X-ray Diffraction†." Langmuir 25, no. 7 (April 7, 2009): 3999–4008. http://dx.doi.org/10.1021/la802768q.

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Barauskas, Justas, Camilla Cervin, Fredrik Tiberg, and Markus Johnsson. "Structure of lyotropic self-assembled lipid nonlamellar liquid crystals and their nanoparticles in mixtures of phosphatidyl choline and α-tocopherol (vitamin E)." Physical Chemistry Chemical Physics 10, no. 43 (2008): 6483. http://dx.doi.org/10.1039/b811251g.

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Basañez, Gorka, Juanita C. Sharpe, Jennifer Galanis, Teresa B. Brandt, J. Marie Hardwick, and Joshua Zimmerberg. "Bax-type Apoptotic Proteins Porate Pure Lipid Bilayers through a Mechanism Sensitive to Intrinsic Monolayer Curvature." Journal of Biological Chemistry 277, no. 51 (October 14, 2002): 49360–65. http://dx.doi.org/10.1074/jbc.m206069200.

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During apoptosis, Bax-type proteins permeabilize the outer mitochondrial membrane to release intermembrane apoptogenic factors into the cytosol via a poorly understood mechanism. We have proposed that Bax and ΔN76Bcl-xL(the Bax-like cleavage fragment of Bcl-xL) function by forming pores that are at least partially composed of lipids (lipidic pore formation). Since the membrane monolayer must bend during lipidic pore formation, we here explore the effect of intrinsic membrane monolayer curvature on pore formation. Nonlamellar lipids with positive intrinsic curvature such as lysophospholipids promoted membrane permeabilization, whereas nonlamellar lipids with negative intrinsic curvature such as diacylglycerol and phosphatidylethanolamine inhibited membrane permeabilization. The differential effects of nonlamellar lipids on membrane permeabilization were not correlated with lipid-induced changes in membrane binding or insertion of Bax or ΔN76Bcl-xL. Altogether, these results are consistent with a model whereby Bax-type proteins change the bending propensity of the membrane to form pores comprised at least in part of lipids in a structure of net positive monolayer curvature.

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Baeza, Isabel, Leopoldo Aguilar, Miguel Ibáñez, Carlos Wong, Francisco Alvarado-Alemán, Carolina Soto, Alejandro Escobar-Gutiérrez, Ricardo Mondragón, and Sirenia González. "Identification of phosphatidate nonlamellar phases on liposomes by flow cytometry." Biochemistry and Cell Biology 73, no. 5-6 (May 1, 1995): 289–97. http://dx.doi.org/10.1139/o95-036.

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This study is the first report that demonstrates nonlamellar arrangements, or lipidic particles, of phosphatidate inserted in the lipid bilayer of liposomes using polyclonal antibodies from mice and flow cytometry. Sera immunoreactivity was analyzed using liposomes that displayed smooth bilayers or phosphatidate particles, as shown by electron microscopy. This cytofluorimetric analysis showed that immune mice sera have a specific immunoreactivity with the phosphatidate particles formed by Mn2+, which also cross-reacted with those formed by Ca2+ and with the cardiolipin particles formed by Mn2+. In addition, these immune sera hardly reacted with smooth bilayered liposomes, independently of the lipid composition studied. Thus, this new methodology can be applied to demonstrate nonlamellar molecular arrangements of lipids in biological membranes.Key words: nonlamellar lipid immunogenicity, lipidic particles immunogenicity, liposomes, flow citometry, anti-phospholipid antibodies.

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Lafleur, Michel, Myer Bloom, and Pieter R. Cullis. "Lipid polymorphism and hydrocarbon order." Biochemistry and Cell Biology 68, no. 1 (January 1, 1990): 1–8. http://dx.doi.org/10.1139/o90-001.

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The use of 2H nuclear magnetic resonance for the characterization of the polymorphic behavior of lipids is illustrated. Different lipid phase preferences may be expected to influence the orientational order and its variation along the acyl chains. Several results are presented to support that view. An increase of motional freedom and a redistribution of the order along the acyl chains are observed during the lamellar-to-hexagonal phase transition, showing that the order profile is sensitive to the lipid phase symmetry. In addition, if the preferences for nonlamellar phases are not expressed explicitly, the presence of "nonbilayer" lipids constrained in bilayer environment induces increased hydrocarbon order. This suggests that order parameters of the acyl chains and lipid polymorphic tendencies are intimately related.Key words: lipid, polymorphism, 2H nuclear magnetic resonance, hydrocarbon order.

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Hazel, Jeffrey R., Susan J. McKinley, and Martin F. Gerrits. "Thermal acclimation of phase behavior in plasma membrane lipids of rainbow trout hepatocytes." American Journal of Physiology-Regulatory, Integrative and Comparative Physiology 275, no. 3 (September 1, 1998): R861—R869. http://dx.doi.org/10.1152/ajpregu.1998.275.3.r861.

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The fluorescent probes laurdan (6-dodecanoyl-2-dimethylaminonapthalene) and N-[7-nitrobenz-2-oxa-1,3-diazol-4-yl] dipalmitoyl-l-α-phosphatidylethanolamine (NBD-PE) in addition to Fourier transform infrared spectroscopy (FTIR) were employed to measure the phase behavior and physical properties of hepatocyte plasma membranes isolated from the livers of thermally acclimated (5 and 20°C) rainbow trout ( Oncorhynchus mykiss). The primary objective was to determine the extent to which the phase behavior of membrane lipids is conserved at different growth temperatures. Arrhenius plots of laurdan-generalized polarization revealed a single discontinuity believed to reflect either the onset of the gel-fluid phase transition or the formation of gel phase microdomains, and this discontinuity occurred at significantly higher temperatures in membranes of 20°C (13.2 ± 0.7°C)- than 5°C (7.2 ± 0.1°C)-acclimated trout. Similarly, acclimation from 5 to 20°C increased both the onset temperature (from 2.0 ± 0.3 to 7.2 ± 0.6°C) and the thermal range (from 10.9 ± 0.5 to 16.0 ± 1.0) of the gel-fluid transition as assessed by FTIR. The gel-fluid transition midpoint (approximately −2°C) and completion temperatures (−9°C) were unchanged by thermal acclimation. The anisotropy of NBD-PE fluorescence displayed a distinct minimum in membranes of both warm- and cold-acclimated trout (reflecting alterations in lipid packing that in pure lipid membranes ultimately lead to the formation of nonlamellar phases) in the range of 56–58°C; only membranes of 5°C-acclimated trout displayed an additional minimum at significantly lower temperatures (24.5 ± 1.7°C). Collectively, these data suggest that the regulation of both the temperature at which gel phase lipids begin to form in response to cooling as well as the propensity of membrane lipids to form nonlamellar phases at higher temperatures may be key features of membrane organization subject to adaptive regulation.

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Koynova, Rumiana. "Lipid Phases Eye View to Lipofection. Cationic Phosphatidylcholine Derivatives as Efficient DNA Carriers for Gene Delivery." Lipid Insights 2 (January 2008): LPI.S864. http://dx.doi.org/10.4137/lpi.s864.

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Efficient delivery of genetic material to cells is needed for tasks of utmost importance in laboratory and clinic, such as gene transfection and gene silencing. Synthetic cationic lipids can be used as delivery vehicles for nucleic acids and are now considered the most promising non-viral gene carriers. They form complexes (lipoplexes) with the polyanionic nucleic acids. A critical obstacle for clinical application of the lipid-mediated DNA delivery (lipofection) is its unsatisfactory efficiency for many cell types. Understanding the mechanism of lipid-mediated DNA delivery is essential for their successful application, as well as for rational design and synthesis of novel cationic lipoid compounds for enhanced gene delivery. According to the current understanding, the critical factor in lipid-mediated transfection is the structural evolution of lipoplexes within the cell, upon interacting and mixing with cellular lipids. In particular, recent studies with cationic phosphatidylcholine derivatives showed that the phase evolution of lipoplex lipids upon interaction and mixing with membrane lipids appears to be decisive for transfection success: specifically, lamellar lipoplex formulations, which were readily susceptible to undergoing lamellar-nonlamellar (precisely lamellar-cubic) phase transition upon mixing with cellular lipids, were found rather consistently associated with superior transfection potency, presumably as a result of facilitated DNA release subsequent to lipoplex fusion with the cellular membranes. Further, hydrophobic moiety of the cationic phospholipids was found able to strongly modulate liposomal gene delivery into primary human umbilical artery endothelial cells; superior activity was found for cationic phosphatidylcholine derivatives with two 14-carbon atom monounsaturated hydrocarbon chains, able to induce formation of cubic phase in membranes. Thus, understanding the lipoplex structure and the phase changes upon interacting with membrane lipids is important for the rational design and successful application of cationic lipids as superior nucleotide delivery agents.

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Lindblom, Goeran, Aake Wieslander, Mats Sjoelund, Goeran Wikander, and Aeke Wieslander. "Phase equilibria of membrane lipids for Acholeplasma laidlawii: importance of a single lipid forming nonlamellar phases." Biochemistry 25, no. 23 (November 18, 1986): 7502–10. http://dx.doi.org/10.1021/bi00371a037.

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Nguyen, Thi-Thao-Linh, and Van-An Duong. "Solid Lipid Nanoparticles." Encyclopedia 2, no. 2 (May 18, 2022): 952–73. http://dx.doi.org/10.3390/encyclopedia2020063.

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Solid lipid nanoparticles (SLNs) are produced from physiologically biocompatible lipids. They have been proven to improve solubility, cellular uptake, and stability, reduce enzyme degradation, and prolong the circulation time of various drugs. SLNs have been applied in the oral, parenteral, transdermal, intranasal, ocular, and pulmonary drug delivery of different drugs, with enhanced safety, bioavailability, and overall therapeutic effects. In this entry, the authors summarize the primary features of SLNs, methods to prepare SLNs, and recent applications of SLNs in drug delivery. Owing to their advantages, SLNs are potential drug delivery systems to improve the management of various diseases and will, soon, be available for clinical use.

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Meanwell, Michael W., Connor O’Sullivan, Perry Howard, and Thomas M. Fyles. "Branched-chain and dendritic lipids for nanoparticles." Canadian Journal of Chemistry 95, no. 2 (February 2017): 120–29. http://dx.doi.org/10.1139/cjc-2016-0462.

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Lipid nanoparticles (LNPs) for drug-delivery applications are largely derived from natural lipids. Synthetic lipids, particularly those incorporating branched hydrocarbons and hyper-branched hydrocarbon architectures, may afford enhanced lipophilicity with enhanced fluidity and thereby lead to LNP stabilization. Hydrocarbon anchors based on serinol diesters were prepared from linear Cn (n = 14, 16, 18) and branched (n = 16) acids with Boc-protected serinol. These diesters were further dimerized on an iminodiacetamide backbone to provide eight branched-chain and dendritic lipid anchors. Derivatization of these core structures provided eight PEG-lipids and seven thiopurine linked lipid–drug conjugates. LNPs were prepared by microfluidic mixing from mixed lipids in ethanol diluted into aqueous media. The lipid–drug conjugates incorporated 5 mol% of a phosphocholine and 5 mol% of a commercial PEG-lipid to form LNPs with a thiopurine drug loading of 15 wt%. The PEG–lipids prepared were formulated at 1.5 mol% as a surface stabilizer to LNPs containing dsDNA lipoplexes. The stability of the LNPs was assessed under different storage conditions through monitoring of particle size. For both LNPs from lipid–thiopurine conjugates and the PEG-lipid systems, there is strong preliminary evidence that hydrocarbon branching results in LNP stabilization. Four of the lipid–drug conjugate formulations were stable to cell culture conditions (10% serum, 37 °C) and the toxicity of these LNPs was assessed in two cell lines relative to the free thiopurines in the medium. The observed toxicity is consistent with cellular uptake of the LNPs and reductive release of the cargo thiopurine within the cell.

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Tenchov, Boris G., Li Wang, Rumiana Koynova, and Robert C. MacDonald. "Modulation of a membrane lipid lamellar–nonlamellar phase transition by cationic lipids: A measure for transfection efficiency." Biochimica et Biophysica Acta (BBA) - Biomembranes 1778, no. 10 (October 2008): 2405–12. http://dx.doi.org/10.1016/j.bbamem.2008.07.022.

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Berger, Manon, Manon Degey, Jeanne Leblond Chain, Erik Maquoi, Brigitte Evrard, Anna Lechanteur, and Géraldine Piel. "Effect of PEG Anchor and Serum on Lipid Nanoparticles: Development of a Nanoparticles Tracking Method." Pharmaceutics 15, no. 2 (February 10, 2023): 597. http://dx.doi.org/10.3390/pharmaceutics15020597.

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Polyethylene glycol (PEG) is used in Lipid Nanoparticles (LNPs) formulations to confer stealth properties and is traditionally anchored in membranes by a lipid moiety whose length significantly impacts the LNPs fate in vivo. C18 acyl chains are efficiently anchored in the membrane, while shorter C14 lipids are quickly desorbed and replaced by a protein corona responsible for the completely different fate of LNPs. In this context, a method to predict the biological behavior of LNPs depending on the lipid-PEG dissociation was developed using the Nanoparticle Tracking Analysis (NTA) method in serum. Two formulations of siRNA-containing LNPs were prepared including CSL3 or SM-102 lipids and were grafted with different lipids-PEG (C18, C14 lipids-PEG, and Ceramide-PEG). The impact of the lipid-PEG on the interactions between LNPs and serum components was demonstrated by monitoring the mean particle size and the concentration over time. In vitro, these formulations demonstrated low toxicity and efficient gene knockdown on tumor MDA-MB-231 cells, but serum was found to significantly impact the efficiency of C18-PEG-based LNPs, while it did not impact the efficiency of C14-PEG-based LNPs. The NTA method demonstrated the ability to discriminate between the behaviors of LNPs according to serum proteins’ interactions. CSL3 lipid and Cer-PEG were confirmed to have promise for LNP formulation.

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Clemente, Ilaria, Stefania Lamponi, Gabriella Tamasi, Liliana Rodolfi, Claudio Rossi, and Sandra Ristori. "Structuring and De-Structuring of Nanovectors from Algal Lipids: Simulated Digestion, Preliminary Antioxidant Capacity and In Vitro Tests." Pharmaceutics 14, no. 9 (September 1, 2022): 1847. http://dx.doi.org/10.3390/pharmaceutics14091847.

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Biocompatible nanocarriers can be obtained by lipid extraction from natural sources such as algal biomasses, which accumulate different lipid classes depending on the employed culture media. Lipid aggregates can be distinguished according to supramolecular architecture into lamellar and nonlamellar structures. This distinction is mainly influenced by the lipid class and molecular packing parameter, which determine the possible values of interfacial curvature and thus the supramolecular symmetries that can be obtained. The nanosystems prepared from bio-sources are able to self-assemble into different compartmentalized structures due to their complex composition. They also present the advantage of increased carrier-target biocompatibility and are suitable to encapsulate and vehiculate poorly water-soluble compounds, e.g., natural antioxidants. Their functional properties stem from the interplay of several parameters. Following previous work, here the functionality of two series of structurally distinct lipid nanocarriers, namely liposomes and cubosomes deriving from algal biomasses with different lipid composition, is characterized. In the view of their possible use as pharmaceutical or nutraceutical formulations, both types of nanovectors were loaded with three well-known antioxidants, i.e., curcumin, α-tocopherol and piperine, and their carrier efficacy was compared considering their different structures. Firstly, carrier stability in biorelevant conditions was assessed by simulating a gastrointestinal tract model. Then, by using an integrated chemical and pharmacological approach, the functionality in terms of encapsulation efficiency, cargo bioaccessibility and kinetics of antioxidant capacity by UV-Visible spectroscopy was evaluated. Subsequently, in vitro cytotoxicity and viability tests after administration to model cell lines were performed. As a consequence of this investigation, it is possible to conclude that nanovectors from algal lipids, i.e., cubosomes and liposomes, can be efficient delivery agents for lipophilic antioxidants, being able to preserve and enhance their activity toward different targets while promoting sustained release.

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Gretskaya, Nataliya, Mikhail Akimov, Dmitry Andreev, Anton Zalygin, Ekaterina Belitskaya, Galina Zinchenko, Elena Fomina-Ageeva, Ilya Mikhalyov, Elena Vodovozova, and Vladimir Bezuglov. "Multicomponent Lipid Nanoparticles for RNA Transfection." Pharmaceutics 15, no. 4 (April 20, 2023): 1289. http://dx.doi.org/10.3390/pharmaceutics15041289.

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Despite the wide variety of available cationic lipid platforms for the delivery of nucleic acids into cells, the optimization of their composition has not lost its relevance. The purpose of this work was to develop multi-component cationic lipid nanoparticles (LNPs) with or without a hydrophobic core from natural lipids in order to evaluate the efficiency of LNPs with the widely used cationic lipoid DOTAP (1,2-dioleoyloxy-3-[trimethylammonium]-propane) and the previously unstudied oleoylcholine (Ol-Ch), as well as the ability of LNPs containing GM3 gangliosides to transfect cells with mRNA and siRNA. LNPs containing cationic lipids, phospholipids and cholesterol, and surfactants were prepared according to a three-stage procedure. The average size of the resulting LNPs was 176 nm (PDI 0.18). LNPs with DOTAP mesylate were more effective than those with Ol-Ch. Core LNPs demonstrated low transfection activity compared with bilayer LNPs. The type of phospholipid in LNPs was significant for the transfection of MDA-MB-231 and SW 620 cancer cells but not HEK 293T cells. LNPs with GM3 gangliosides were the most efficient for the delivery of mRNA to MDA-MB-231 cells and siRNA to SW620 cells. Thus, we developed a new lipid platform for the efficient delivery of RNA of various sizes to mammalian cells.

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Ramezanpour, M., M. L. Schmidt, I. Bodnariuc, J. A. Kulkarni, S. S. W. Leung, P. R. Cullis, J. L. Thewalt, and D. P. Tieleman. "Ionizable amino lipid interactions with POPC: implications for lipid nanoparticle function." Nanoscale 11, no. 30 (2019): 14141–46. http://dx.doi.org/10.1039/c9nr02297j.

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The distribution of ionizable amino lipids (KC2) is critical in structure of lipid nanoparticles, siRNA entrapment and endosomal release. Neutral KC2 segregates from phospholipids (POPC) and forms an oily core in the bilayer interior.

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Dobreva, Mirena, Stefan Stefanov, and Velichka Andonova. "Natural Lipids as Structural Components of Solid Lipid Nanoparticles and Nanostructured Lipid Carriers for Topical Delivery." Current Pharmaceutical Design 26, no. 36 (October 23, 2020): 4524–35. http://dx.doi.org/10.2174/1381612826666200514221649.

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Background: Solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC) are useful drug delivery systems for dermal application. Thanks to their biocompatible and biodegradable profile, these carriers offer many advantages such as enhanced bioavailability, low toxicity, viable drug targeting and controlled release. SLN and NLC are composed of well-tolerated lipids, including natural fats and oils that are successfully used in the pharmaceutical and cosmetic dermal formulation. Objective: This article presents an overview of the benefits of selecting natural fats and oils as structural components of SLN and NLC for topical application. Methods: This review is based on data published over the past 20 years about the development of stable and nontoxic lipid nanoparticles with natural lipids. We shed light on the role of natural fats in skin restoration, as well as on the contributed penetration and occlusive properties of SLN and NLC. Results: The deliberate selection of excipients (type and lipid ratio) influences the quality of the final dermal formulation. Natural lipids show good compatibility with different active molecules and are able to create stable lipid matrices that facilitate the biopharmaceutical properties of lipid nanoparticles. Patents involving natural fats and oils in SLN and NLC composition are listed, yet it is important to note that the approved marketed formulations are mainly cosmetic, not pharmaceutical, products. Conclusion: Natural lipids can enhance topical drug delivery by adding their ability of improving skin penetration and hydration to the permeation and occlusion properties of SLN and NLC.

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Basso, João, Maria Mendes, Tânia Cova, João Sousa, Alberto Pais, Ana Fortuna, Rui Vitorino, and Carla Vitorino. "A Stepwise Framework for the Systematic Development of Lipid Nanoparticles." Biomolecules 12, no. 2 (January 27, 2022): 223. http://dx.doi.org/10.3390/biom12020223.

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A properly designed nanosystem aims to deliver an optimized concentration of the active pharmaceutical ingredient (API) at the site of action, resulting in a therapeutic response with reduced adverse effects. Due to the vast availability of lipids and surfactants, producing stable lipid dispersions is a double-edged sword: on the one hand, the versatility of composition allows for a refined design and tuning of properties; on the other hand, the complexity of the materials and their physical interactions often result in laborious and time-consuming pre-formulation studies. However, how can they be tailored, and which premises are required for a “right at first time” development? Here, a stepwise framework encompassing the sequential stages of nanoparticle production for disulfiram delivery is presented. Drug in lipid solubility analysis leads to the selection of the most suitable liquid lipids. As for the solid lipid, drug partitioning studies point out the lipids with increased capacity for solubilizing and entrapping disulfiram. The microscopical evaluation of the physical compatibility between liquid and solid lipids further indicates the most promising core compositions. The impact of the outer surfactant layer on the colloidal properties of the nanosystems is evaluated recurring to machine learning algorithms, in particular, hierarchical clustering, principal component analysis, and partial least squares regression. Overall, this work represents a comprehensive systematic approach to nanoparticle formulation studies that serves as a basis for selecting the most suitable excipients that comprise solid lipid nanoparticles and nanostructured lipid carriers.

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Korzun, Tetiana, Abraham S. Moses, Parham Diba, Ariana L. Sattler, Olena R. Taratula, Gaurav Sahay, Oleh Taratula, and Daniel L. Marks. "From Bench to Bedside: Implications of Lipid Nanoparticle Carrier Reactogenicity for Advancing Nucleic Acid Therapeutics." Pharmaceuticals 16, no. 8 (July 31, 2023): 1088. http://dx.doi.org/10.3390/ph16081088.

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In biomedical applications, nanomaterial-based delivery vehicles, such as lipid nanoparticles, have emerged as promising instruments for improving the solubility, stability, and encapsulation of various payloads. This article provides a formal review focusing on the reactogenicity of empty lipid nanoparticles used as delivery vehicles, specifically emphasizing their application in mRNA-based therapies. Reactogenicity refers to the adverse immune responses triggered by xenobiotics, including administered lipid nanoparticles, which can lead to undesirable therapeutic outcomes. The key components of lipid nanoparticles, which include ionizable lipids and PEG-lipids, have been identified as significant contributors to their reactogenicity. Therefore, understanding the relationship between lipid nanoparticles, their structural constituents, cytokine production, and resultant reactogenic outcomes is essential to ensure the safe and effective application of lipid nanoparticles in mRNA-based therapies. Although efforts have been made to minimize these adverse reactions, further research and standardization are imperative. By closely monitoring cytokine profiles and assessing reactogenic manifestations through preclinical and clinical studies, researchers can gain valuable insights into the reactogenic effects of lipid nanoparticles and develop strategies to mitigate undesirable reactions. This comprehensive review underscores the importance of investigating lipid nanoparticle reactogenicity and its implications for the development of mRNA–lipid nanoparticle therapeutics in various applications beyond vaccine development.

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Bala, Tripura Sundari I., and C. V. S. Subramanyam. "Formulation and Evaluation of Lipid Based Nanoparticles of Etravirine." Journal of Drug Delivery and Therapeutics 14, no. 1 (January 15, 2024): 79–90. http://dx.doi.org/10.22270/jddt.v14i1.6373.

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Engineered nanoparticles have the potential to revolutionize the diagnosis and treatment of many diseases like HIV/AIDS. Etravirine is one of the key components of highly active antiretroviral therapy used for the treatment of HIV-1 infections. The aim of the present study was to formulate and evaluate nanostructured lipid carriers of etravirine, intended for targeted delivery to macrophages, using solvent emulsification - evaporation technique. Estimates of drug solubility were employed for selection of solid lipids, liquid lipids and stabilizers for the preparation of NLCs. Design of experiments was used to optimize the formulation with respect to drug-lipid ratio and concentration of stabilizer in the external phase using 32 full factorial design. Particle size of the carriers and drug release characteristics were the responses which were set to suitable levels for optimization. The optimized formulation was prepared and characterized for size, poly dispersity index, zeta potential, entrapment efficiency and appearance. The nanostructured lipid carriers of etravirine were prepared using stearylamine and glyceryl monostearate as solid lipids, Capryol 90 as liquid lipid and polyvinyl pyrrolidone as stabilizer. All experimental batches showed high drug loading efficiencies nearing 99%, indicating that etravirine remained closely associated with the lipids. The nanostructured lipid carriers displayed a zeta potential of -10.1 mv and a particle size of 261.6 nm with a polydispersity index of 0.374. In vitro release of etravirine from the optimized formulation at 2 h was 9% indicative of a low burst; and 56% of the entrapped drug was released after 24 h, suggesting prolonged release characteristics. Thus, etravirine loaded lipidic nanoparticles with potential for targeting cellular reservoirs of the AIDS virus such as macrophages were successfully developed. Keywords: Etravirine, Nanostructured lipid carriers, full factorial design

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Yu, Linwen. "Principle and Application of Lipid Nanoparticles in Cosmetics." Applied and Computational Engineering 24, no. 1 (November 7, 2023): 231–36. http://dx.doi.org/10.54254/2755-2721/24/20230714.

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Lipid nanoparticles (LNs) are colloidal particles having a biocompatible lipid matrix and nanoparticle (NP) sizes between 100 nm and 400 nm. They are called "nanosafe" carriers and show outstanding tolerability. Solid lipid nanoparticles use lipid as the skeleton material which has a high melting point. SLNs have the characteristics of high physical stability, relatively less drug leakage and good slow release, low toxicity and easy to mass production. The structure of the solid particle matrix allows solid lipid nanoparticles (SLNs) to be distinguished from nanostructured lipid carriers (NLCs). NLC is prepared by mixing liquid lipids and solid lipids. NLC improves the solubility of the active substance, improves the release ability of the substance, and also prolongs the storage life of the active substance in the carrier. Plenty of characteristics for skin application of pharmaceuticals and cosmetics are displayed by SLNs and NLC, such as drug targeting, regulated release of active ingredients, occlusion properties, and related enhancements to penetration and skin hydration. This review focuses on the characteristic of SLNs and NLCS, analyzing their advantages and disadvantages and lipid nanoparticles application in cosmetics are described in detail.

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Severino, Patrícia, Tatiana Andreani, Ana Sofia Macedo, Joana F. Fangueiro, Maria Helena A. Santana, Amélia M. Silva, and Eliana B. Souto. "Current State-of-Art and New Trends on Lipid Nanoparticles (SLN and NLC) for Oral Drug Delivery." Journal of Drug Delivery 2012 (November 24, 2012): 1–10. http://dx.doi.org/10.1155/2012/750891.

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Lipids and lipid nanoparticles are extensively employed as oral-delivery systems for drugs and other active ingredients. These have been exploited for many features in the field of pharmaceutical technology. Lipids usually enhance drug absorption in the gastrointestinal tract (GIT), and when formulated as nanoparticles, these molecules improve mucosal adhesion due to small particle size and increasing their GIT residence time. In addition, lipid nanoparticles may also protect the loaded drugs from chemical and enzymatic degradation and gradually release drug molecules from the lipid matrix into blood, resulting in improved therapeutic profiles compared to free drug. Therefore, due to their physiological and biodegradable properties, lipid molecules may decrease adverse side effects and chronic toxicity of the drug-delivery systems when compared to other of polymeric nature. This paper highlights the importance of lipid nanoparticles to modify the release profile and the pharmacokinetic parameters of drugs when administrated through oral route.

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Wang, Ming, John A. Zuris, Fantao Meng, Holly Rees, Shuo Sun, Pu Deng, Yong Han, et al. "Efficient delivery of genome-editing proteins using bioreducible lipid nanoparticles." Proceedings of the National Academy of Sciences 113, no. 11 (February 29, 2016): 2868–73. http://dx.doi.org/10.1073/pnas.1520244113.

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A central challenge to the development of protein-based therapeutics is the inefficiency of delivery of protein cargo across the mammalian cell membrane, including escape from endosomes. Here we report that combining bioreducible lipid nanoparticles with negatively supercharged Cre recombinase or anionic Cas9:single-guide (sg)RNA complexes drives the electrostatic assembly of nanoparticles that mediate potent protein delivery and genome editing. These bioreducible lipids efficiently deliver protein cargo into cells, facilitate the escape of protein from endosomes in response to the reductive intracellular environment, and direct protein to its intracellular target sites. The delivery of supercharged Cre protein and Cas9:sgRNA complexed with bioreducible lipids into cultured human cells enables gene recombination and genome editing with efficiencies greater than 70%. In addition, we demonstrate that these lipids are effective for functional protein delivery into mouse brain for gene recombination in vivo. Therefore, the integration of this bioreducible lipid platform with protein engineering has the potential to advance the therapeutic relevance of protein-based genome editing.

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Wilhelmy, Christoph, Isabell Sofia Keil, Lukas Uebbing, Martin A. Schroer, Daniel Franke, Thomas Nawroth, Matthias Barz, et al. "Polysarcosine-Functionalized mRNA Lipid Nanoparticles Tailored for Immunotherapy." Pharmaceutics 15, no. 8 (August 1, 2023): 2068. http://dx.doi.org/10.3390/pharmaceutics15082068.

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Lipid nanoparticles (LNPs) have gained great attention as carriers for mRNA-based therapeutics, finding applications in various indications, extending beyond their recent use in vaccines for infectious diseases. However, many aspects of LNP structure and their effects on efficacy are not well characterized. To further exploit the potential of mRNA therapeutics, better control of the relationship between LNP formulation composition with internal structure and transfection efficiency in vitro is necessary. We compared two well-established ionizable lipids, namely DODMA and MC3, in combination with two helper lipids, DOPE and DOPC, and two polymer-grafted lipids, either with polysarcosine (pSar) or polyethylene glycol (PEG). In addition to standard physicochemical characterization (size, zeta potential, RNA accessibility), small-angle X-ray scattering (SAXS) was used to analyze the structure of the LNPs. To assess biological activity, we performed transfection and cell-binding assays in human peripheral blood mononuclear cells (hPBMCs) using Thy1.1 reporter mRNA and Cy5-labeled mRNA, respectively. With the SAXS measurements, we were able to clearly reveal the effects of substituting the ionizable and helper lipid on the internal structure of the LNPs. In contrast, pSar as stealth moieties affected the LNPs in a different manner, by changing the surface morphology towards higher roughness. pSar LNPs were generally more active, where the highest transfection efficiency was achieved with the LNP formulation composition of MC3/DOPE/pSar. Our study highlights the utility of pSar for improved mRNA LNP products and the importance of pSar as a novel stealth moiety enhancing efficiency in future LNP formulation development. SAXS can provide valuable information for the rational development of such novel formulations by elucidating structural features in different LNP compositions.

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Kavita Rani, Amit Kumar J. Raval, Dinesh Kaushik, and Rajesh Khathuriya. "Formulation of Nanostructured lipid particles." Asian Pacific Journal of Nursing and Health Sciences 3, no. 2 (December 30, 2020): 20–24. http://dx.doi.org/10.46811/apjnh/3.2.4.

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Lipid nanocarriers are developed as an alternative to polymeric nanoparticles, liposomes and emulsions. NLCs are the second generation lipid carriers developed to overcome problems associated with Solid Lipid Nanoparticles and are utilized in various therapeutic approaches. NLCs were used for the delivery of lipophilic drugs .Biocompatible nature of lipids is responsible for its development as a good drug delivery. It was found to be having excellent characteristics over other lipid formulations.

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Mo, Kyumin, Ayoung Kim, Soohyun Choe, Miyoung Shin, and Hyunho Yoon. "Overview of Solid Lipid Nanoparticles in Breast Cancer Therapy." Pharmaceutics 15, no. 8 (July 31, 2023): 2065. http://dx.doi.org/10.3390/pharmaceutics15082065.

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Lipid nanoparticles (LNPs), composed of ionized lipids, helper lipids, and cholesterol, provide general therapeutic effects by facilitating intracellular transport and avoiding endosomal compartments. LNP-based drug delivery has great potential for the development of novel gene therapies and effective vaccines. Solid lipid nanoparticles (SLNs) are derived from physiologically acceptable lipid components and remain robust at body temperature, thereby providing high structural stability and biocompatibility. By enhancing drug delivery through blood vessels, SLNs have been used to improve the efficacy of cancer treatments. Breast cancer, the most common malignancy in women, has a declining mortality rate but remains incurable. Recently, as an anticancer drug delivery system, SLNs have been widely used in breast cancer, improving the therapeutic efficacy of drugs. In this review, we discuss the latest advances of SLNs for breast cancer treatment and their potential in clinical use.

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Chacko, Juna B., Gudanagaram R. Vijayasankar, Bendi S. Venkateswarlu, and Margret C. Rajappa. "MECHANISTIC OUTCOMES OF LIPID CORE ON SOLID LIPID NANOPARTICLE CHARACTERIZATION." INDIAN DRUGS 61, no. 02 (February 28, 2024): 35–42. http://dx.doi.org/10.53879/id.61.02.13881.

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In our present study, solid lipid nanoparticles were fabricated by modified double emulsification followed by ultracentrifugation method. The SLNs of the anti-HIV drugs lamivudine, tenofovir disoproxil fumarate and efavirenz were synthesized using lipids Compritol 888 ATO, glyceryl monostearate, stearic acid and emulsifiers soy lecithin and Pluronic®F68. The synthesized SLNs were characterized for compatibility studies, mean particle size, PDI, zeta potential, surface morphology and entrapment studies. The higher amount of Compritol based SLNs formulation showed maximum entrapment efficiency with comparatively larger sized, homogenous particles. All the lipid based SLNs possessed no incompatibilities and showed high stability profiles. Based on the results of surface morphology, zeta potential and high entrapment efficiency values, the optimum lipid for SLNs formulation among the other lipids was determined to be Compritol 888 ATO.

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V. More, Apoorva, Bharat V. Dhokchawle, Savita J. Tauro, and Savita V. Kulkarni. "LIPID AS AN EXCIPIENT FOR DESIGN AND DEVELOPMENT OF FORMULATIONS." Indian Drugs 59, no. 07 (September 16, 2022): 7–20. http://dx.doi.org/10.53879/id.59.07.12199.

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Lipids are present abundantly in human body in several forms. Different types of lipids are available with diverse physical properties, based on which suitable lipids can be selected for development of formulations. Lipids are also available for specific purposes like lubrication, emulsification, emollientes and enhancement of bioavailability. Conventionally, many lipids are used in formulation of tablets, capsules, emulsions and cosmetics. In recent years, use of lipids for drug delivery has been extended to Solid Lipid Nanoparticles (SLN), Nanostructured Lipid Carriers (NLC), and Self-Micro Emulsifying Drug Delivery System (SEDDS), which are emerging technologies designed to address challenges like solubility and bioavailability of poorly water-soluble drugs. This paper mainly focuses on different types of formulations in which lipids are used, and parameters which are critical for selection of lipid in any dosage form development. Several examples are quoted for different uses of lipids. Finally challenges in use of lipids and regulatory aspects are discussed.

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Chime, Salome A., Paul A. Akpa, and Anthony A. Attama. "The Utility of Lipids as Nanocarriers and Suitable Vehicle in Pharmaceutical Drug Delivery." Current Nanomaterials 4, no. 3 (November 11, 2019): 160–75. http://dx.doi.org/10.2174/2405461504666191016091827.

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Lipid based excipients have gained popularity recently in the formulation of drugs in order to improve their pharmacokinetic profiles. For drugs belonging to the Biopharmaceutics Classification System (BCS) class II and IV, lipid excipients play vital roles in improving their pharmacokinetics properties. Various nanocarriers viz: Solid lipid nanoparticles, nanostructured lipid carriers, selfnanoemulsifying drug delivery systems (SNEDDS), nanoliposomes and liquid crystal nanoparticles have been employed as delivery systems for such drugs with evident successes. Lipid-based nanotechnology have been used to control the release of drugs and have utility for drug targeting and hence, have been used for the delivery of various anticancer drugs and for colon targeting. Drugs encapsulated in lipids have enhanced stability due to the protection they enjoy in the lipid core of these nanoformulations. However, lipid excipients could be influenced by factors which could affect the physicochemical properties of lipid-based drug delivery systems (LBDDS). These factors include the liquid crystalline phase transition, lipid crystallization and polymorphism amongst others. However, some of the physicochemical properties of lipids made them useful as nanocarriers in the formulation of various nanoformulations. Lipids form vesicles of bilayer which have been used to deliver drugs and are often referred to as liposomes and nanoliposomes. This work aims at reviewing the different classes of lipid excipients used in formulating LBDDS and nanoformulations. Also, some factors that influence the properties of lipids, different polymorphic forms in lipid excipients that made them effective nanocarriers in nano-drug delivery would be discussed. Special considerations in selecting lipid excipients used in formulating various forms of nanoformulations would be discussed.

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Medjmedj, Ayoub, Albert Ngalle-Loth, Rudy Clemençon, Josef Hamacek, Chantal Pichon, and Federico Perche. "In Cellulo and In Vivo Comparison of Cholesterol, Beta-Sitosterol and Dioleylphosphatidylethanolamine for Lipid Nanoparticle Formulation of mRNA." Nanomaterials 12, no. 14 (July 17, 2022): 2446. http://dx.doi.org/10.3390/nano12142446.

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Lipid Nanoparticles (LNPs) are a leading class of mRNA delivery systems. LNPs are made of an ionizable lipid, a polyethyleneglycol (PEG)-lipid conjugate and helper lipids. The success of LNPs is due to proprietary ionizable lipids and appropriate helper lipids. Using a benchmark lipid (D-Lin-MC3) we compared the ability of three helper lipids to transfect dendritic cells in cellulo and in vivo. Studies revealed that the choice of helper lipid does not influence the transfection efficiency of immortalized cells but, LNPs prepared with DOPE (dioleylphosphatidylethanolamine) and β-sitosterol were more efficient for mRNA transfection in murine dendritic cells than LNPs containing DSPC (distearoylphosphatidylcholine). This higher potency of DOPE and β-sitosterol LNPs for mRNA expression was also evident in vivo but only at low mRNA doses. Overall, these data provide valuable insight for the design of novel mRNA LNP vaccines.

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Eichmann, Cédric, Stefan Bibow, and Roland Riek. "α-Synuclein lipoprotein nanoparticles." Nanotechnology Reviews 6, no. 1 (February 1, 2017): 105–10. http://dx.doi.org/10.1515/ntrev-2016-0062.

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AbstractApolipoprotein nanodiscs are a versatile tool in nanotechnology as membrane mimetics allowing, for example, the study of membrane proteins. It has recently been discovered that the Parkinson’s disease associated protein α-synuclein (α-Syn) can also form discoid-like lipoprotein nanoparticles. The present review highlights the observation that α-Syn has the properties to define stable and homogeneous populations of nanoparticles with diameters of 7–10 nm and 19–28 nm by modifying lipid vesicles or encapsulating lipid bilayers in a nanodisc-type fashion, respectively. In contrast to apolipoprotein nanodiscs, α-Syn nanoparticles can incorporate entirely negatively charged lipids emphasizing their potential use in nanotechnology as a negatively charged membrane mimetic.

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Musielak, Ewelina, Agnieszka Feliczak-Guzik, and Izabela Nowak. "Synthesis and Potential Applications of Lipid Nanoparticles in Medicine." Materials 15, no. 2 (January 17, 2022): 682. http://dx.doi.org/10.3390/ma15020682.

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Currently, carriers of active ingredients in the form of particles of a size measured in nanometers are the focus of interest of research centers worldwide. So far, submicrometer emulsions, liposomes, as well as microspheres, and nanospheres made of biodegradable polymers have been used in medicine. Recent studies show particular interest in nanoparticles based on lipids, and at the present time, are even referred to as the “era of lipid carriers”. With the passage of time, lipid nanoparticles of the so-called first and second generation, SLN (Solid Lipid Nanoparticles) and nanostructured lipid carriers and NLC (Nanostructured Lipid Carriers), respectively, turned out to be an alternative for all imperfections of earlier carriers. These carriers are characterized by a number of beneficial functional properties, including, among others, structure based on lipids well tolerated by the human body, high stability, and ability to carry hydro- and lipophilic compounds. Additionally, these carriers can enhance the distribution of the drug in the target organ and alter the pharmacokinetic properties of the drug carriers to enhance the medical effect and minimize adverse side effects. This work is focused on the current review of the state-of-the-art related to the synthesis and applications of popular nanoparticles in medicine, with a focus on their use, e.g., in COVID-19 vaccines.

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Quach, Hung, Tuong-Vi Le, Thanh-Thuy Nguyen, Phuong Nguyen, Cuu Khoa Nguyen, and Le Hang Dang. "Nano-Lipids Based on Ginger Oil and Lecithin as a Potential Drug Delivery System." Pharmaceutics 14, no. 8 (August 9, 2022): 1654. http://dx.doi.org/10.3390/pharmaceutics14081654.

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Lipid nanoparticles based on lecithin are an interesting part of drug delivery systems. However, the stability of lecithin nano-lipids is problematic due to the degradation of lecithin, causing a decrease in pH. In this study, the modification of the conventional nano-lipid-based soybean lecithin was demonstrated. Ginger-oil-derived Zingiber officinale was used along with lecithin, cholesterol and span 80 to fabricate nano-lipids (GL nano-lipids) using a thin-film method. TEM and a confocal microscope were used to elucidate GL nano-lipids’ liposome-like morphology. The average size of the resultant nano-lipid was 249.1 nm with monodistribution (PDI = 0.021). The ζ potential of GL nano-lipids was negative, similarly to as-prepared nano-lipid-based lecithin. GL nano-lipid were highly stable over 60 days of storage at room temperature in terms of size and ζ potential. A shift in pH value from alkaline to acid was detected in lecithin nano-lipids, while with the incorporation of ginger oil, the pH value of nano-lipid dispersion was around 7.0. Furthermore, due to the richness of shogaol-6 and other active compounds in ginger oil, the GL nano-lipid was endowed with intrinsic antibacterial activity. In addition, the sulforhodamine B (SRB) assay and live/dead imaging revealed the excellent biocompatibility of GL nano-lipids. Notably, GL nano-lipids were capable of carrying hydrophobic compounds such as curcumin and performed a pH-dependent release profile. A subsequent characterization showed their suitable potential for drug delivery systems.

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Lewis, Daniel R., Latrisha K. Petersen, Adam W. York, Kyle R. Zablocki, Laurie B. Joseph, Vladyslav Kholodovych, Robert K. Prud’homme, Kathryn E. Uhrich, and Prabhas V. Moghe. "Sugar-based amphiphilic nanoparticles arrest atherosclerosis in vivo." Proceedings of the National Academy of Sciences 112, no. 9 (February 17, 2015): 2693–98. http://dx.doi.org/10.1073/pnas.1424594112.

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Atherosclerosis, the build-up of occlusive, lipid-rich plaques in arterial walls, is a focal trigger of chronic coronary, intracranial, and peripheral arterial diseases, which together account for the leading causes of death worldwide. Although the directed treatment of atherosclerotic plaques remains elusive, macrophages are a natural target for new interventions because they are recruited to lipid-rich lesions, actively internalize modified lipids, and convert to foam cells with diseased phenotypes. In this work, we present a nanomedicine platform to counteract plaque development based on two building blocks: first, at the single macrophage level, sugar-based amphiphilic macromolecules (AMs) were designed to competitively block oxidized lipid uptake via scavenger receptors on macrophages; second, for sustained lesion-level intervention, AMs were fabricated into serum-stable core/shell nanoparticles (NPs) to rapidly associate with plaques and inhibit disease progression in vivo. An AM library was designed and fabricated into NP compositions that showed high binding and down-regulation of both MSR1 and CD36 scavenger receptors, yielding minimal accumulation of oxidized lipids. When intravenously administered to a mouse model of cardiovascular disease, these AM NPs showed a pronounced increase in lesion association compared with the control nanoparticles, causing a significant reduction in neointimal hyperplasia, lipid burden, cholesterol clefts, and overall plaque occlusion. Thus, synthetic macromolecules configured as NPs are not only effectively mobilized to lipid-rich lesions but can also be deployed to counteract atheroinflammatory vascular diseases, highlighting the promise of nanomedicines for hyperlipidemic and metabolic syndromes.

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Yu, Xiaojuan, Chuanfei Yu, Xiaohong Wu, Yu Cui, Xiaoda Liu, Yan Jin, Yuhua Li, and Lan Wang. "Validation of an HPLC-CAD Method for Determination of Lipid Content in LNP-Encapsulated COVID-19 mRNA Vaccines." Vaccines 11, no. 5 (May 4, 2023): 937. http://dx.doi.org/10.3390/vaccines11050937.

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Lipid nanoparticles (LNPs) are widely used as delivery systems for mRNA vaccines. The stability and bilayer fluidity of LNPs are determined by the properties and contents of the various lipids used in the formulation system, and the delivery efficiency of LNPs largely depends on the lipid composition. For the quality control of such vaccines, here we developed and validated an HPLC-CAD method to identify and determine the contents of four lipids in an LNP-encapsulated COVID-19 mRNA vaccine to support lipid analysis for the development of new drugs and vaccines.

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P, Ashok Kumar, Mancy S.P., Manjunath K, Suresh V. Kulkarni, and Jagadeesh R. "Formulation and Evaluation of Fluvoxamine Maleate Loaded Lipid Nanoparticle." International Journal of Pharmaceutical Sciences and Nanotechnology 12, no. 4 (July 31, 2019): 4593–600. http://dx.doi.org/10.37285/ijpsn.2019.12.4.5.

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Recently solid lipid nanoparticles (SLN's) have been received much attention by the researchers owing to its biodegradability, bioavailability and the ability to deliver wide range of drugs to the targeted site of action. The purpose of the present study is to develop and evaluate the fluvoxamine maleate loaded lipid nanoparticles. The fluvoxamine maleate lipid nanoparticles (LN’s) were prepared by the hot melt homogenization followed by the sonication by using different combination of lipids like tristearin, compritol, olive oil, coconut oil, sesame oil. Compatibility study was confirmed by FTIR and DSC. The LN’s were evaluated for particle size, PDI, zeta potential, entrapment efficiency and in-vitro drug release. For the Fluvoxamine maleate LN’s prepared using the solid lipids, the particle size ranged from 98.58 to 152.43 nm. PDI of all formulations were good within the range of 0.239 to 0.456 with zeta potential from - 6.52 to -18.6 mV. Entrapment efficiency observed was in the range of 64.56 to 84.23 %. The cumulative percentage release of fluvoxamine maleate from different LN’s varied from 46.14 to 81.48%. For the formulations prepared using the combination of solid lipids and liquid lipids, Fluvoxamine maleate LN’s the particle size ranged from 63.22 to 263.8 nm. With good PDI range from 0.229 to 0.514 Zeta potential of all formulation is from - 5.01 to -9.30 mV. Entrapment efficiency observed was in the range of 71.02 to 90.51 %. The cumulative percentage release of fluvoxamine maleate from different LN’s varied from 63.71 to 85.41% depending upon the drug lipid ratio, the type of lipid used. The release kinetic studies showed that the release was first order, diffusion controlled, and the ‘n’ values obtained from the Korsmeyer-Peppa’s model indicated the release mechanism was Anomalous (non-Fickian) diffusion type.

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Lee, Kwahun, and Yan Yu. "Lipid bilayer disruption induced by amphiphilic Janus nanoparticles: the non-monotonic effect of charged lipids." Soft Matter 15, no. 11 (2019): 2373–80. http://dx.doi.org/10.1039/c8sm02525h.

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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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Berzenina, O. V., D. E. Kytova, A. V. Shtemenko, and N. I. Shtemenko. "Surface lipids of Kalanhoe as a material for nanoparticles preparation." Voprosy Khimii i Khimicheskoi Tekhnologii, no. 3 (May 2021): 57–63. http://dx.doi.org/10.32434/0321-4095-2021-136-3-57-63.

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The purpose of the investigation was to elaborate the methods of extraction of surface lipids from Kalanchoe Degremona plants and preparation of solid lipid nanoparticles containing a dirhenium(III) cluster compound. The procedure of growing plants and increasing the quantity of surface lipids by means of adaptation biochemistry to toxicants was used in this work. Data on the quantities of extracts, IR-spectra, and GC-MS-data of hydrocarbons and oxocompounds of surface lipids obtained were presented. An increase in the total number of surface lipids and an insignificant change in heterogeneity under the influence of monochlorobenzene exposition were shown. The absence of differences in the ratio of the intensity of the characteristic bands in the FTIR spectra allowed concluding that the toxicant did not affect the qualitative composition of the surface lipids. The nanoparticles (with a size of 14540 nm) with high encapsulation efficiency were prepared, these nanoparticles containing the dirhenium(III) cluster compound that previously showed a cytostatic action in experiments in vivo.

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Peng, Congnan, Qian Zhang, Jian-an Liu, Zhen-peng Wang, Zhen-wen Zhao, Ning Kang, Yuxin Chen, and Qing Huo. "Study on titanium dioxide nanoparticles as MALDI MS matrix for the determination of lipids in the brain." Green Processing and Synthesis 10, no. 1 (January 1, 2021): 700–710. http://dx.doi.org/10.1515/gps-2021-0056.

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Abstract The structures of lipids are diverse, and thus, lipids show various biological functions. Systematic determination of lipids in organisms has always been a concern. In this paper, a methodology on the matrix-assisted laser desorption ionization mass spectrometry (MALDI MS), with titanium dioxide nanoparticles (TiO2 NPs) as the matrix, was studied for lipid determination. The results showed that the following conditions were preferable in the determination of small-molecule lipids (such as hypoxanthine, guanosine, uridine, and cytidine), lipid standards (such as GC, GM, TG, phosphatidylethanolamine, phosphatidylcholine, and ceramide), and mixed lipids (extracted from brain homogenate with methanol alone and with the B&D method): TiO2 NPs as the matrix, absolute ethanol as the solvent, 1 mg of TiO2 NPs dispersed in 1 mL of absolute ethanol as the matrix solution, NaCl as the ionization reagent, and positive mass spectrometry (MS) as the mode. Modified TiO2 NP as a new matrix for MALDI MS will be a future research direction; in addition, the characteristics of TiO2 NPs make it a potential matrix for imaging MS.

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Hu, Guangxia, Hui Yin, Chunxiang Li, Suxiu Ng, Xi Jiang Yin, and Gong Hao. "Investigation of Lanolin Lipid-Based Nanoparticles as Carriers for Avobenzone." Nano LIFE 10, no. 04 (October 12, 2020): 2040011. http://dx.doi.org/10.1142/s1793984420400115.

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The aim of this study is to develop and characterize lanolin lipid-based nanoparticles as carriers for avobenzone. Solid Lipid nanoparticles (SLNs) were prepared by the high-pressure homogenization technique. The influence of emulsifiers, avobenzone content in lipid (0–20[Formula: see text]wt.%), solid lipid blends’ composition and dispersions’ solid content on nanoparticles size, zeta potentials, PI value, stability, matrix structure and UV absorption were investigated. The matrix structure of the lipids and the blends was investigated by using X-ray diffraction (XRD) techniques. The particle sizes were [Formula: see text]200[Formula: see text]nm and PI values are below 0.25 after production. The stability of lipid nanoparticles (LNs) was characterized by naked eye and dynamic light scattering (DLS) technique. The optimized lipid is the lanolin nanostructured lipid carrier with lecithin and APG 810 as co-emulsifiers.

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Kuboyama, Takeshi, Kaori Yagi, Tomoyuki Naoi, Tomohiro Era, Nobuhiro Yagi, Yoshisuke Nakasato, Hayato Yabuuchi, et al. "Simplifying the Chemical Structure of Cationic Lipids for siRNA-Lipid Nanoparticles." ACS Medicinal Chemistry Letters 10, no. 5 (April 12, 2019): 749–53. http://dx.doi.org/10.1021/acsmedchemlett.8b00652.

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Gilbert, Jennifer, Anna Fornell, Najet Mahmoudi, Ann Terry, and Tommy Nylander. "Lipid nanoparticles using cationic ionisable lipids: Effect of cargo on structure." Biophysical Journal 122, no. 3 (February 2023): 222a. http://dx.doi.org/10.1016/j.bpj.2022.11.1322.

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Sedlmayr, Viktor Laurin, Silvia Schobesberger, Sarah Spitz, Peter Ertl, David Johannes Wurm, Julian Quehenberger, and Oliver Spadiut. "Archaeal ether lipids improve internalization and transfection with mRNA lipid nanoparticles." European Journal of Pharmaceutics and Biopharmaceutics 197 (April 2024): 114213. http://dx.doi.org/10.1016/j.ejpb.2024.114213.

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Hangargekar, Sachin Raosaheb, Pradeepkumar Mohanty, and Ashish Jain. "Solid Lipid Nanoparticles for Brain Targeting." Journal of Drug Delivery and Therapeutics 9, no. 6-s (December 15, 2019): 248–52. http://dx.doi.org/10.22270/jddt.v9i6-s.3783.

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Abstract:

Brain is considered to be highly impermeable barrier, possessing different obstacles like presence of enzymes, presence of tight junctions that limit the entry for most of the drugs. The presence of these obstacles, possess a challenge for administration of the drugs. The conventional means of drug delivery in form of emulsions, fail to overcome these obstacles, and hence there is a need for newer drug delivery approach, that will cross these barriers of the brain. So, these nanoparticles can be an alternative to other conventional systems. They offer several advantages such as improved bioavailability and solubility that are composed of macromolecular materials like lipids and polymers possess low cytotoxicity, high drug loading capability, and good scalability these are the most effective colloidal carriers that have the ability to incorporate drugs into nanocarriers and used as drug targeting to specific area. Thus, this article will emphasise on properties of Blood Brain Barrier, strategies to overcome the blood–brain barrier, literature regarding the use of SLNs in various neurological disease states, production methods of SLN and its evaluation. Hence, these solid lipid formulations can be a new form and one of the promising approach for drug delivery system in future, that have remarkable possibility to cross the BBB. Keywords: Solid lipid nanoparticles, Nanocarriers, Blood–brain barrier

Journal articles on the topic 'Lipid nanoparticles of nonlamellar lipids'

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