Enhanced oral bioavailability of silymarin using liposomes containing a bile salt: preparation by supercritical fluid technology and evaluation in vitro and in vivo

Gang Yang,1 Yaping Zhao,2 Yongtai Zhang,1 Beilei Dang,1 Ying Liu,1 Nianping Feng11School of Pharmacy, Shanghai University of Traditional Chinese Medicine, 2School of Chemistry and Chemical Engineering, Shanghai Jiao Tong University, Shanghai, People’s Republic of ChinaAbstract: The aim of...

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Autores principales:	Yang G, Zhao YP, Zhang YT, Dang BL, Liu Y, Feng NP
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2015
Materias:	Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/ff48052510bc4d9c89b6a7f066c83db3
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spelling	oai:doaj.org-article:ff48052510bc4d9c89b6a7f066c83db32021-12-02T03:05:26ZEnhanced oral bioavailability of silymarin using liposomes containing a bile salt: preparation by supercritical fluid technology and evaluation in vitro and in vivo1178-2013https://doaj.org/article/ff48052510bc4d9c89b6a7f066c83db32015-10-01T00:00:00Zhttps://www.dovepress.com/enhanced-oral-bioavailability-of-silymarin-using-liposomes-containing--peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Gang Yang,1 Yaping Zhao,2 Yongtai Zhang,1 Beilei Dang,1 Ying Liu,1 Nianping Feng11School of Pharmacy, Shanghai University of Traditional Chinese Medicine, 2School of Chemistry and Chemical Engineering, Shanghai Jiao Tong University, Shanghai, People’s Republic of ChinaAbstract: The aim of this investigation was to develop a procedure to improve the dissolution and bioavailability of silymarin (SM) by using bile salt-containing liposomes that were prepared by supercritical fluid technology (ie, solution-enhanced dispersion by supercritical fluids [SEDS]). The process for the preparation of SM-loaded liposomes containing a bile salt (SM-Lip-SEDS) was optimized using a central composite design of response surface methodology with the ratio of SM to phospholipids (w/w), flow rate of solution (mL/min), and pressure (MPa) as independent variables. Particle size, entrapment efficiency (EE), and drug loading (DL) were dependent variables for optimization of the process and formulation variables. The particle size, zeta potential, EE, and DL of the optimized SM-Lip-SEDS were 160.5 nm, -62.3 mV, 91.4%, and 4.73%, respectively. Two other methods to produce SM liposomes were compared to the SEDS method. The liposomes obtained by the SEDS method exhibited the highest EE and DL, smallest particle size, and best stability compared to liposomes produced by the thin-film dispersion and reversed-phase evaporation methods. Compared to the SM powder, SM-Lip-SEDS showed increased in vitro drug release. The in vivo AUC0-t of SM-Lip-SEDS was 4.8-fold higher than that of the SM powder. These results illustrate that liposomes containing a bile salt can be used to enhance the oral bioavailability of SM and that supercritical fluid technology is suitable for the preparation of liposomes.Keywords: silymarin, solution-enhanced dispersion by supercritical fluids, liposomes, bile salt, bioavailabilityYang GZhao YPZhang YTDang BLLiu YFeng NPDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2015, Iss default, Pp 6633-6644 (2015)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine (General) R5-920
spellingShingle	Medicine (General) R5-920 Yang G Zhao YP Zhang YT Dang BL Liu Y Feng NP Enhanced oral bioavailability of silymarin using liposomes containing a bile salt: preparation by supercritical fluid technology and evaluation in vitro and in vivo
description	Gang Yang,1 Yaping Zhao,2 Yongtai Zhang,1 Beilei Dang,1 Ying Liu,1 Nianping Feng11School of Pharmacy, Shanghai University of Traditional Chinese Medicine, 2School of Chemistry and Chemical Engineering, Shanghai Jiao Tong University, Shanghai, People’s Republic of ChinaAbstract: The aim of this investigation was to develop a procedure to improve the dissolution and bioavailability of silymarin (SM) by using bile salt-containing liposomes that were prepared by supercritical fluid technology (ie, solution-enhanced dispersion by supercritical fluids [SEDS]). The process for the preparation of SM-loaded liposomes containing a bile salt (SM-Lip-SEDS) was optimized using a central composite design of response surface methodology with the ratio of SM to phospholipids (w/w), flow rate of solution (mL/min), and pressure (MPa) as independent variables. Particle size, entrapment efficiency (EE), and drug loading (DL) were dependent variables for optimization of the process and formulation variables. The particle size, zeta potential, EE, and DL of the optimized SM-Lip-SEDS were 160.5 nm, -62.3 mV, 91.4%, and 4.73%, respectively. Two other methods to produce SM liposomes were compared to the SEDS method. The liposomes obtained by the SEDS method exhibited the highest EE and DL, smallest particle size, and best stability compared to liposomes produced by the thin-film dispersion and reversed-phase evaporation methods. Compared to the SM powder, SM-Lip-SEDS showed increased in vitro drug release. The in vivo AUC0-t of SM-Lip-SEDS was 4.8-fold higher than that of the SM powder. These results illustrate that liposomes containing a bile salt can be used to enhance the oral bioavailability of SM and that supercritical fluid technology is suitable for the preparation of liposomes.Keywords: silymarin, solution-enhanced dispersion by supercritical fluids, liposomes, bile salt, bioavailability
format	article
author	Yang G Zhao YP Zhang YT Dang BL Liu Y Feng NP
author_facet	Yang G Zhao YP Zhang YT Dang BL Liu Y Feng NP
author_sort	Yang G
title	Enhanced oral bioavailability of silymarin using liposomes containing a bile salt: preparation by supercritical fluid technology and evaluation in vitro and in vivo
title_short	Enhanced oral bioavailability of silymarin using liposomes containing a bile salt: preparation by supercritical fluid technology and evaluation in vitro and in vivo
title_full	Enhanced oral bioavailability of silymarin using liposomes containing a bile salt: preparation by supercritical fluid technology and evaluation in vitro and in vivo
title_fullStr	Enhanced oral bioavailability of silymarin using liposomes containing a bile salt: preparation by supercritical fluid technology and evaluation in vitro and in vivo
title_full_unstemmed	Enhanced oral bioavailability of silymarin using liposomes containing a bile salt: preparation by supercritical fluid technology and evaluation in vitro and in vivo
title_sort	enhanced oral bioavailability of silymarin using liposomes containing a bile salt: preparation by supercritical fluid technology and evaluation in vitro and in vivo
publisher	Dove Medical Press
publishDate	2015
url	https://doaj.org/article/ff48052510bc4d9c89b6a7f066c83db3
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_version_	1718402019798024192

Enhanced oral bioavailability of silymarin using liposomes containing a bile salt: preparation by supercritical fluid technology and evaluation in vitro and in vivo

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