Liposomes containing bile salts as novel ocular delivery systems for tacrolimus (FK506): in vitro characterization and improved corneal permeation

Yikang Dai,1 Rui Zhou,2 Lin Liu,1 Yi Lu,2 Jianping Qi,2 Wei Wu21Department of Ophthalmology, Renji Hospital, School of Medicine, Shanghai Jiaotong University, 2Key Laboratory of Smart Drug Delivery, Ministry of Education and PLA, School of Pharmacy, Fudan University, Shanghai, People's Repub...

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Autores principales:	Dai Y, Zhou R, Liu L, Lu Y, Qi J, Wu W
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2013
Materias:	Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/87b4c25ba91e40119d9c6475744d8df2
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spelling	oai:doaj.org-article:87b4c25ba91e40119d9c6475744d8df22021-12-02T02:29:50ZLiposomes containing bile salts as novel ocular delivery systems for tacrolimus (FK506): in vitro characterization and improved corneal permeation1176-91141178-2013https://doaj.org/article/87b4c25ba91e40119d9c6475744d8df22013-05-01T00:00:00Zhttp://www.dovepress.com/liposomes-containing-bile-salts-as-novel-ocular-delivery-systems-for-t-a13045https://doaj.org/toc/1176-9114https://doaj.org/toc/1178-2013Yikang Dai,1 Rui Zhou,2 Lin Liu,1 Yi Lu,2 Jianping Qi,2 Wei Wu21Department of Ophthalmology, Renji Hospital, School of Medicine, Shanghai Jiaotong University, 2Key Laboratory of Smart Drug Delivery, Ministry of Education and PLA, School of Pharmacy, Fudan University, Shanghai, People's Republic of ChinaAbstract: The objective of this study was to investigate the potential of liposomes containing bile salts as an ophthalmic delivery system for tacrolimus to improve corneal permeability. Liposomes containing bile salts, including sodium taurocholate, sodium deoxycholate, and sodium glycocholate, were produced by the thin-film dispersion method with a particle size of approximately 100 nm and an entrapment efficiency of more than 90%. Less than 5% tacrolimus was released from conventional liposomes and from liposomes containing sodium taurocholate, sodium deoxycholate, or sodium glycocholate over 12 hours. The cellular uptake of conventional liposomes was significantly higher than that of liposomes containing bile salts. However, liposomes containing bile salts exerted a 3–4-fold increase of tacrolimus in ex vivo corneal transport of tacrolimus compared with conventional liposomes. When rabbit eyes were treated with a DiI perchlorate-loaded liposome suspension, liposomes containing bile salts showed fast and sustained penetration across the cornea. Unfortunately, liposomes containing sodium deoxycholate caused toxicity or irritation to both spontaneously derived human corneal epithelial cells and the rabbit cornea. Therefore, liposomes containing sodium taurocholate and sodium glycocholate are potential carriers in ocular drug delivery systems, given their low toxicity and vastly improved permeability.Keywords: liposomes, bile salt, tacrolimus, cornea, sodium taurocholate, sodium deoxycholate, sodium glycocholateDai YZhou RLiu LLu YQi JWu WDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2013, Iss default, Pp 1921-1933 (2013)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine (General) R5-920
spellingShingle	Medicine (General) R5-920 Dai Y Zhou R Liu L Lu Y Qi J Wu W Liposomes containing bile salts as novel ocular delivery systems for tacrolimus (FK506): in vitro characterization and improved corneal permeation
description	Yikang Dai,1 Rui Zhou,2 Lin Liu,1 Yi Lu,2 Jianping Qi,2 Wei Wu21Department of Ophthalmology, Renji Hospital, School of Medicine, Shanghai Jiaotong University, 2Key Laboratory of Smart Drug Delivery, Ministry of Education and PLA, School of Pharmacy, Fudan University, Shanghai, People's Republic of ChinaAbstract: The objective of this study was to investigate the potential of liposomes containing bile salts as an ophthalmic delivery system for tacrolimus to improve corneal permeability. Liposomes containing bile salts, including sodium taurocholate, sodium deoxycholate, and sodium glycocholate, were produced by the thin-film dispersion method with a particle size of approximately 100 nm and an entrapment efficiency of more than 90%. Less than 5% tacrolimus was released from conventional liposomes and from liposomes containing sodium taurocholate, sodium deoxycholate, or sodium glycocholate over 12 hours. The cellular uptake of conventional liposomes was significantly higher than that of liposomes containing bile salts. However, liposomes containing bile salts exerted a 3–4-fold increase of tacrolimus in ex vivo corneal transport of tacrolimus compared with conventional liposomes. When rabbit eyes were treated with a DiI perchlorate-loaded liposome suspension, liposomes containing bile salts showed fast and sustained penetration across the cornea. Unfortunately, liposomes containing sodium deoxycholate caused toxicity or irritation to both spontaneously derived human corneal epithelial cells and the rabbit cornea. Therefore, liposomes containing sodium taurocholate and sodium glycocholate are potential carriers in ocular drug delivery systems, given their low toxicity and vastly improved permeability.Keywords: liposomes, bile salt, tacrolimus, cornea, sodium taurocholate, sodium deoxycholate, sodium glycocholate
format	article
author	Dai Y Zhou R Liu L Lu Y Qi J Wu W
author_facet	Dai Y Zhou R Liu L Lu Y Qi J Wu W
author_sort	Dai Y
title	Liposomes containing bile salts as novel ocular delivery systems for tacrolimus (FK506): in vitro characterization and improved corneal permeation
title_short	Liposomes containing bile salts as novel ocular delivery systems for tacrolimus (FK506): in vitro characterization and improved corneal permeation
title_full	Liposomes containing bile salts as novel ocular delivery systems for tacrolimus (FK506): in vitro characterization and improved corneal permeation
title_fullStr	Liposomes containing bile salts as novel ocular delivery systems for tacrolimus (FK506): in vitro characterization and improved corneal permeation
title_full_unstemmed	Liposomes containing bile salts as novel ocular delivery systems for tacrolimus (FK506): in vitro characterization and improved corneal permeation
title_sort	liposomes containing bile salts as novel ocular delivery systems for tacrolimus (fk506): in vitro characterization and improved corneal permeation
publisher	Dove Medical Press
publishDate	2013
url	https://doaj.org/article/87b4c25ba91e40119d9c6475744d8df2
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Liposomes containing bile salts as novel ocular delivery systems for tacrolimus (FK506): in vitro characterization and improved corneal permeation

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