Self-microemulsifying drug-delivery system for improved oral bioavailability of probucol: preparation and evaluation

Xianyi Sha, Juan Wu, Yanzuo Chen, Xiaoling FangKey Laboratory of Smart Drug Delivery (Fudan University), Ministry of Education and PLA, Department of Pharmaceutics, School of Pharmacy, Fudan University, Shanghai, ChinaAbstract: The objective of our investigation was to design a self-microemulsifying...

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Autores principales:	Sha X, Wu J, Chen Y, Fang X
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2012
Materias:	Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/de80322be0cd48d4b0bdd1b2a4720e21
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spelling	oai:doaj.org-article:de80322be0cd48d4b0bdd1b2a4720e212021-12-02T00:39:10ZSelf-microemulsifying drug-delivery system for improved oral bioavailability of probucol: preparation and evaluation1176-91141178-2013https://doaj.org/article/de80322be0cd48d4b0bdd1b2a4720e212012-02-01T00:00:00Zhttp://www.dovepress.com/self-microemulsifying-drug-delivery-system-for-improved-oral-bioavaila-a9239https://doaj.org/toc/1176-9114https://doaj.org/toc/1178-2013Xianyi Sha, Juan Wu, Yanzuo Chen, Xiaoling FangKey Laboratory of Smart Drug Delivery (Fudan University), Ministry of Education and PLA, Department of Pharmaceutics, School of Pharmacy, Fudan University, Shanghai, ChinaAbstract: The objective of our investigation was to design a self-microemulsifying drug-delivery system (SMEDDS) to improve the bioavailability of probucol. SMEDDS was composed of probucol, olive oil, Lauroglycol FCC, Cremophor EL, Tween-80, and PEG-400. Droplet sizes were determined. In vitro release was investigated. Pharmacokinetics and bioavailability of probucol suspension, oil solution, and SMEDDS were evaluated and compared in rats. Plasma drug concentration was determined by high-performance liquid chromatography. After administration of probucol suspension, plasma drug concentration was very low. Relative bioavailability of SMEDDS was dramatically enhanced in an average of 2.15- and 10.22-fold that of oil solution and suspension, respectively. It was concluded that bioavailability of probucol was enhanced greatly by SMEDDS. Improved solubility and lymphatic transport may contribute to the enhancement of bioavailability.Keywords: self-microemulsifying drug-delivery system (SMEDDS), probucol, bioavailabilitySha XWu JChen YFang XDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2012, Iss default, Pp 705-712 (2012)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine (General) R5-920
spellingShingle	Medicine (General) R5-920 Sha X Wu J Chen Y Fang X Self-microemulsifying drug-delivery system for improved oral bioavailability of probucol: preparation and evaluation
description	Xianyi Sha, Juan Wu, Yanzuo Chen, Xiaoling FangKey Laboratory of Smart Drug Delivery (Fudan University), Ministry of Education and PLA, Department of Pharmaceutics, School of Pharmacy, Fudan University, Shanghai, ChinaAbstract: The objective of our investigation was to design a self-microemulsifying drug-delivery system (SMEDDS) to improve the bioavailability of probucol. SMEDDS was composed of probucol, olive oil, Lauroglycol FCC, Cremophor EL, Tween-80, and PEG-400. Droplet sizes were determined. In vitro release was investigated. Pharmacokinetics and bioavailability of probucol suspension, oil solution, and SMEDDS were evaluated and compared in rats. Plasma drug concentration was determined by high-performance liquid chromatography. After administration of probucol suspension, plasma drug concentration was very low. Relative bioavailability of SMEDDS was dramatically enhanced in an average of 2.15- and 10.22-fold that of oil solution and suspension, respectively. It was concluded that bioavailability of probucol was enhanced greatly by SMEDDS. Improved solubility and lymphatic transport may contribute to the enhancement of bioavailability.Keywords: self-microemulsifying drug-delivery system (SMEDDS), probucol, bioavailability
format	article
author	Sha X Wu J Chen Y Fang X
author_facet	Sha X Wu J Chen Y Fang X
author_sort	Sha X
title	Self-microemulsifying drug-delivery system for improved oral bioavailability of probucol: preparation and evaluation
title_short	Self-microemulsifying drug-delivery system for improved oral bioavailability of probucol: preparation and evaluation
title_full	Self-microemulsifying drug-delivery system for improved oral bioavailability of probucol: preparation and evaluation
title_fullStr	Self-microemulsifying drug-delivery system for improved oral bioavailability of probucol: preparation and evaluation
title_full_unstemmed	Self-microemulsifying drug-delivery system for improved oral bioavailability of probucol: preparation and evaluation
title_sort	self-microemulsifying drug-delivery system for improved oral bioavailability of probucol: preparation and evaluation
publisher	Dove Medical Press
publishDate	2012
url	https://doaj.org/article/de80322be0cd48d4b0bdd1b2a4720e21
work_keys_str_mv	AT shax selfmicroemulsifyingdrugdeliverysystemforimprovedoralbioavailabilityofprobucolpreparationandevaluation AT wuj selfmicroemulsifyingdrugdeliverysystemforimprovedoralbioavailabilityofprobucolpreparationandevaluation AT cheny selfmicroemulsifyingdrugdeliverysystemforimprovedoralbioavailabilityofprobucolpreparationandevaluation AT fangx selfmicroemulsifyingdrugdeliverysystemforimprovedoralbioavailabilityofprobucolpreparationandevaluation
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Self-microemulsifying drug-delivery system for improved oral bioavailability of probucol: preparation and evaluation

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