Enhanced absorption of hydroxysafflor yellow A using a self-double-emulsifying drug delivery system: in vitro and in vivo studies

Liang-Zhong Lv,1 Chen-Qi Tong,1 Qing Lv,2,3 Xin-Jiang Tang,2 Li-Ming Li,2 Qing-Xia Fang,1 Jia Yu,1 Min Han,2 Jian-Qing Gao21Department of Pharmacy, Zhejiang Provincial People&#39;s Hospital, 2Institute of Pharmaceutics, College of Pharmaceutical Sciences, Zhejiang University, 3Pharmaceutics...

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Autores principales:	Lv Q, Lv LZ, Tong CQ, Tang XJ, Li LM, Fang QX, Yu J, Han M, Gao JQ
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2012
Materias:	Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/6aaea2059d644d32acb3639f23f34f16
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spelling	oai:doaj.org-article:6aaea2059d644d32acb3639f23f34f162021-12-02T00:35:30ZEnhanced absorption of hydroxysafflor yellow A using a self-double-emulsifying drug delivery system: in vitro and in vivo studies1176-91141178-2013https://doaj.org/article/6aaea2059d644d32acb3639f23f34f162012-07-01T00:00:00Zhttp://www.dovepress.com/enhanced-absorption-of-hydroxysafflor-yellow-a-using-a-self-double-emu-a10549https://doaj.org/toc/1176-9114https://doaj.org/toc/1178-2013Liang-Zhong Lv,1 Chen-Qi Tong,1 Qing Lv,2,3 Xin-Jiang Tang,2 Li-Ming Li,2 Qing-Xia Fang,1 Jia Yu,1 Min Han,2 Jian-Qing Gao21Department of Pharmacy, Zhejiang Provincial People&#39;s Hospital, 2Institute of Pharmaceutics, College of Pharmaceutical Sciences, Zhejiang University, 3Pharmaceutics Laboratory of TCM, ZheJiang Traditional Chinese Medicine University, Hangzhou, ChinaAbstract: Hydroxysafflor yellow A (HSYA), the main active ingredient of the safflower plant (Carthamus tinctorius L.), is a hydrophilic drug with low oral bioavailability. Water-in-oil-in-water (w/o/w) double emulsions may enhance the oral absorption of HSYA. In this study, we prepared a self-double-emulsifying drug delivery system (SDEDDS) to improve the absorption of HSYA. SDEDDS consists of water in oil emulsions and hydrophilic surfactants that can self-emulsify into w/o/w double emulsions in the aqueous gastrointestinal environment. Confocal laser scanning micrographs showed that spherical droplets were uniformly distributed in the dispersion medium with narrow particle size distribution and could form fine w/o/w double emulsions upon dilution in dispersion medium with gentle stirring. The dispersed oil droplets contained small dispersed aqueous droplets consistent with the characteristics of double emulsions. Furthermore, in vitro cellular experiments were performed to study the mechanism of the absorption promoting effect of SDEDDS. The accumulation of rhodamine-123 in Caco-2 cells was used to evaluate the efflux transport of p-glycoprotein inhibitor. Histopathologic studies on the rat intestine showed that SDEDDS can cause mucosal damage to a certain degree of toxicity, however this was not serious. These results suggest that SDEDDS can greatly improve the oral absorption of HSYA. Given the toxicity demonstrated to the small intestine, the formulation prescription should be improved to enhance security in the future.Keywords: self-double-emulsifying drug delivery system, hydroxysafflor yellow A, Caco-2 cells, bioavailability, histopathologic studiesLv QLv LZTong CQTang XJLi LMFang QXYu JHan MGao JQDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2012, Iss default, Pp 4099-4107 (2012)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine (General) R5-920
spellingShingle	Medicine (General) R5-920 Lv Q Lv LZ Tong CQ Tang XJ Li LM Fang QX Yu J Han M Gao JQ Enhanced absorption of hydroxysafflor yellow A using a self-double-emulsifying drug delivery system: in vitro and in vivo studies
description	Liang-Zhong Lv,1 Chen-Qi Tong,1 Qing Lv,2,3 Xin-Jiang Tang,2 Li-Ming Li,2 Qing-Xia Fang,1 Jia Yu,1 Min Han,2 Jian-Qing Gao21Department of Pharmacy, Zhejiang Provincial People&#39;s Hospital, 2Institute of Pharmaceutics, College of Pharmaceutical Sciences, Zhejiang University, 3Pharmaceutics Laboratory of TCM, ZheJiang Traditional Chinese Medicine University, Hangzhou, ChinaAbstract: Hydroxysafflor yellow A (HSYA), the main active ingredient of the safflower plant (Carthamus tinctorius L.), is a hydrophilic drug with low oral bioavailability. Water-in-oil-in-water (w/o/w) double emulsions may enhance the oral absorption of HSYA. In this study, we prepared a self-double-emulsifying drug delivery system (SDEDDS) to improve the absorption of HSYA. SDEDDS consists of water in oil emulsions and hydrophilic surfactants that can self-emulsify into w/o/w double emulsions in the aqueous gastrointestinal environment. Confocal laser scanning micrographs showed that spherical droplets were uniformly distributed in the dispersion medium with narrow particle size distribution and could form fine w/o/w double emulsions upon dilution in dispersion medium with gentle stirring. The dispersed oil droplets contained small dispersed aqueous droplets consistent with the characteristics of double emulsions. Furthermore, in vitro cellular experiments were performed to study the mechanism of the absorption promoting effect of SDEDDS. The accumulation of rhodamine-123 in Caco-2 cells was used to evaluate the efflux transport of p-glycoprotein inhibitor. Histopathologic studies on the rat intestine showed that SDEDDS can cause mucosal damage to a certain degree of toxicity, however this was not serious. These results suggest that SDEDDS can greatly improve the oral absorption of HSYA. Given the toxicity demonstrated to the small intestine, the formulation prescription should be improved to enhance security in the future.Keywords: self-double-emulsifying drug delivery system, hydroxysafflor yellow A, Caco-2 cells, bioavailability, histopathologic studies
format	article
author	Lv Q Lv LZ Tong CQ Tang XJ Li LM Fang QX Yu J Han M Gao JQ
author_facet	Lv Q Lv LZ Tong CQ Tang XJ Li LM Fang QX Yu J Han M Gao JQ
author_sort	Lv Q
title	Enhanced absorption of hydroxysafflor yellow A using a self-double-emulsifying drug delivery system: in vitro and in vivo studies
title_short	Enhanced absorption of hydroxysafflor yellow A using a self-double-emulsifying drug delivery system: in vitro and in vivo studies
title_full	Enhanced absorption of hydroxysafflor yellow A using a self-double-emulsifying drug delivery system: in vitro and in vivo studies
title_fullStr	Enhanced absorption of hydroxysafflor yellow A using a self-double-emulsifying drug delivery system: in vitro and in vivo studies
title_full_unstemmed	Enhanced absorption of hydroxysafflor yellow A using a self-double-emulsifying drug delivery system: in vitro and in vivo studies
title_sort	enhanced absorption of hydroxysafflor yellow a using a self-double-emulsifying drug delivery system: in vitro and in vivo studies
publisher	Dove Medical Press
publishDate	2012
url	https://doaj.org/article/6aaea2059d644d32acb3639f23f34f16
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Enhanced absorption of hydroxysafflor yellow A using a self-double-emulsifying drug delivery system: in vitro and in vivo studies

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