Formulation and Optimization of Lipid Nanoparticles with Chitosan for Quercetin Delivery
Abstract Quercetin presents numerous activities, such as antioxidant, anticancer, cardioprotective, etc. that make it suitable for its therapeutic use. However, quercetin has a limited biodisponibility due to its low water solubility which limits its pharmaceutical application. In this work, the encapsulation of quercetin in chitosan-coated liposomes was proposed. The influence of the molecular weight of chitosan (ultralow, low and medium) and phosphatidylcholine:chitosan ratio (16:1, 8:1, 4:1) on the size, polydispersity index, encapsulation efficiency and zeta potential of the prepared nanoparticles were evaluated, obtaining values of 339.02-670.62 nm, 0,26 y 0,32, 43.5-59.3 % y 55.2-63.3 mV respectively. Subsequently, low molecular weight chitosan and phosphatidylcholine:chitosan 16:1 ratio were selected for a freeze-drying study of the nanoparticles, with freezing temperatures of -20 ºC and -80 ºC and lactose, trehalose and sucrose as cryoprotectants. The encapsulation efficiency and residual moisture were studied. Freezing conditions at -80 ºC and trehalose as cryoprotectant prevented the loss of encapsulated quercetin to a greater extent.
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Mohanraj, VJ, Chen Y. Nanoparticles - A review. Trop. J. Pharm. Res. 2006;5(1):561-573.
Wang W, Sun C, Mao L, Ma P, Liu F, Yang J et al. The biological activities, chemical stability, metabolism and delivery systems of quercetin: A review. Trends Food Sci. 2016;56:21-38.
Barros C de, Aranha N, Severino P, Souto EB, Zielińska A, Lopes A et al. Quality by design approach for the development of liposome carrying ghrelin for intranasal administration. Pharmaceutics. 2021;13(5):686.
Brahmachari G. Natural bioactive molecules: impacts and prospects. Brahmachari G, editor. Alpha Science International Ltd; 2014.
Elkomy MH, Ali AA, Eid HM. Chitosan on the surface of nanoparticles for enhanced drug delivery: A comprehensive review. J Control Release. 2022;351:923-940.
Gorantla S, Wadhwa G, Jain S, Sankar S, Nuwal K, Mahmood A et al. Recent advances in nanocarriers for nutrient delivery. Drug Deliv. Transl. Res. 2022;12(10):2359-2384.
Guimarães D, Noro J, Silva C, Cavaco-Paulo A, Nogueira E. Protective Effect of Saccharides on Freeze-Dried Liposomes Encapsulating Drugs. Front. Bioeng. Biotechnol. 2019;7:424.
Hao J, Guo B, Yu S, Zhang W, Zhang D, Wang J et al. Encapsulation of the flavonoid quercetin with chitosan-coated nano-liposomes. LWT. 2017;85:37-44.
Jiang H, Wang Y, Xu X, Deng L, Feng L, Han J et al. Effect of oligosaccharides as lyoprotectants on the stability of curcumin-loaded nanoliposomes during lyophilization. Food Chem. 2023;410:135436.
Kaşıkcı MB, Bağdatlıoğlu N. Bioavailability of Quercetin. Current Research in Nutrition and Food Science Journal. 25 de octubre de 2016;4:146-151.
Kumar S, Dutta J, Dutta PK, Koh J. A systematic study on chitosan-liposome based systems for biomedical applications. Int. J. Biol. Macromol. 2020;160:470-481.
Lee MK. Liposomes for Enhanced Bioavailability of Water-Insoluble Drugs: In Vivo Evidence and Recent Approaches. Pharmaceutics. 2020;12(3):264.
Mohanraj, VJ, Chen Y. Nanoparticles - A review. Trop. J. Pharm. Res. 2006;5(1):561-573.
Wang W, Sun C, Mao L, Ma P, Liu F, Yang J et al. The biological activities, chemical stability, metabolism and delivery systems of quercetin: A review. Trends Food Sci. 2016;56:21-38.
Gallego, D., & Colino, C. I. (2023). Formulation and Optimization of Lipid Nanoparticles with Chitosan for Quercetin Delivery. FarmaJournal, 8(2), 17–25. https://doi.org/10.14201/fj2023821725
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