Enhanced oral bioavailability of cyclosporine A by liposomes containing a bile salt

Peipei Guan1, Yi Lu1, Jianping Qi1, Mengmeng Niu1, Ruyue Lian1, Fuqiang Hu2, Wei Wu11School of Pharmacy, Fudan University, Shanghai, People&#39;s Republic of China; 2School of Pharmacy, Zhejiang University, Hangzhou, People&#39;s Republic of ChinaAbstract: The main purpose of this st...

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Autores principales:	Guan P, Lu Y, Qi J, Niu M, Lian R, Hu F, Wu W
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2011
Materias:	Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/f363ab10b062485289e35dd15192257f
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spelling	oai:doaj.org-article:f363ab10b062485289e35dd15192257f2021-12-02T06:34:20ZEnhanced oral bioavailability of cyclosporine A by liposomes containing a bile salt1176-91141178-2013https://doaj.org/article/f363ab10b062485289e35dd15192257f2011-05-01T00:00:00Zhttp://www.dovepress.com/enhanced-oral-bioavailability-of-cyclosporine-a-by-liposomes-containin-a7343https://doaj.org/toc/1176-9114https://doaj.org/toc/1178-2013Peipei Guan1, Yi Lu1, Jianping Qi1, Mengmeng Niu1, Ruyue Lian1, Fuqiang Hu2, Wei Wu11School of Pharmacy, Fudan University, Shanghai, People&#39;s Republic of China; 2School of Pharmacy, Zhejiang University, Hangzhou, People&#39;s Republic of ChinaAbstract: The main purpose of this study was to evaluate liposomes containing a bile salt, sodium deoxycholate (SDC), as oral drug delivery systems to enhance the oral bioavailability of the poorly water-soluble and poorly permeable drug, cyclosporine A (CyA). Liposomes composed of soybean phosphatidylcholine (SPC) and SDC were prepared by a thin-film dispersion method followed by homogenization. Several properties of the liposomes including particle size, polydispersity index, and entrapment efficiency were characterized. The in vitro release of CyA from these liposomes was less than 5% at 12 hours as measured by a dynamic dialysis method. The pharmacokinetic results in rats showed improved absorption of CyA in SPC/SDC liposomes, compared with CyA-loaded conventional SPC/cholesterol (Chol) liposomes and microemulsion-based Sandimmune Neoral&reg;. The relative oral bioavailability of CyA-loaded SPC/SDC and SPC/Chol liposomes was 120.3% and 98.6%, respectively, with Sandimmun Neoral as the reference. The enhanced bioavailability of CyA was probably due to facilitated absorption by the liposomes containing SDC rather than improved release rate.Keywords: liposomes, bile salt, sodium deoxycholate, cyclosporine A, oral bioavailabilityGuan PLu YQi JNiu MLian RHu FWu WDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2011, Iss default, Pp 965-974 (2011)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine (General) R5-920
spellingShingle	Medicine (General) R5-920 Guan P Lu Y Qi J Niu M Lian R Hu F Wu W Enhanced oral bioavailability of cyclosporine A by liposomes containing a bile salt
description	Peipei Guan1, Yi Lu1, Jianping Qi1, Mengmeng Niu1, Ruyue Lian1, Fuqiang Hu2, Wei Wu11School of Pharmacy, Fudan University, Shanghai, People&#39;s Republic of China; 2School of Pharmacy, Zhejiang University, Hangzhou, People&#39;s Republic of ChinaAbstract: The main purpose of this study was to evaluate liposomes containing a bile salt, sodium deoxycholate (SDC), as oral drug delivery systems to enhance the oral bioavailability of the poorly water-soluble and poorly permeable drug, cyclosporine A (CyA). Liposomes composed of soybean phosphatidylcholine (SPC) and SDC were prepared by a thin-film dispersion method followed by homogenization. Several properties of the liposomes including particle size, polydispersity index, and entrapment efficiency were characterized. The in vitro release of CyA from these liposomes was less than 5% at 12 hours as measured by a dynamic dialysis method. The pharmacokinetic results in rats showed improved absorption of CyA in SPC/SDC liposomes, compared with CyA-loaded conventional SPC/cholesterol (Chol) liposomes and microemulsion-based Sandimmune Neoral&reg;. The relative oral bioavailability of CyA-loaded SPC/SDC and SPC/Chol liposomes was 120.3% and 98.6%, respectively, with Sandimmun Neoral as the reference. The enhanced bioavailability of CyA was probably due to facilitated absorption by the liposomes containing SDC rather than improved release rate.Keywords: liposomes, bile salt, sodium deoxycholate, cyclosporine A, oral bioavailability
format	article
author	Guan P Lu Y Qi J Niu M Lian R Hu F Wu W
author_facet	Guan P Lu Y Qi J Niu M Lian R Hu F Wu W
author_sort	Guan P
title	Enhanced oral bioavailability of cyclosporine A by liposomes containing a bile salt
title_short	Enhanced oral bioavailability of cyclosporine A by liposomes containing a bile salt
title_full	Enhanced oral bioavailability of cyclosporine A by liposomes containing a bile salt
title_fullStr	Enhanced oral bioavailability of cyclosporine A by liposomes containing a bile salt
title_full_unstemmed	Enhanced oral bioavailability of cyclosporine A by liposomes containing a bile salt
title_sort	enhanced oral bioavailability of cyclosporine a by liposomes containing a bile salt
publisher	Dove Medical Press
publishDate	2011
url	https://doaj.org/article/f363ab10b062485289e35dd15192257f
work_keys_str_mv	AT guanp enhancedoralbioavailabilityofcyclosporineabyliposomescontainingabilesalt AT luy enhancedoralbioavailabilityofcyclosporineabyliposomescontainingabilesalt AT qij enhancedoralbioavailabilityofcyclosporineabyliposomescontainingabilesalt AT nium enhancedoralbioavailabilityofcyclosporineabyliposomescontainingabilesalt AT lianr enhancedoralbioavailabilityofcyclosporineabyliposomescontainingabilesalt AT huf enhancedoralbioavailabilityofcyclosporineabyliposomescontainingabilesalt AT wuw enhancedoralbioavailabilityofcyclosporineabyliposomescontainingabilesalt
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Enhanced oral bioavailability of cyclosporine A by liposomes containing a bile salt

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