Mechanism of enhanced oral absorption of hydrophilic drug incorporated in hydrophobic nanoparticles

Liang-Zhong Lv,1 Chen-Qi Tong,1 Jia Yu,1 Min Han,2 Jian-Qing Gao21Department of Pharmacy, Zhejiang Provincial People's Hospital, Hangzhou, People's Republic of China; 2Institute of Pharmaceutics, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, People's Repu...

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Autores principales:	Lv LZ, Tong CQ, Yu J, Han M, Gao JQ
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2013
Materias:	Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/86a3bfe23b1149639f00c4cceb064f52
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spelling	oai:doaj.org-article:86a3bfe23b1149639f00c4cceb064f522021-12-02T07:14:15ZMechanism of enhanced oral absorption of hydrophilic drug incorporated in hydrophobic nanoparticles1176-91141178-2013https://doaj.org/article/86a3bfe23b1149639f00c4cceb064f522013-07-01T00:00:00Zhttp://www.dovepress.com/mechanism-of-enhanced-oral-absorption-of-hydrophilic-drug-incorporated-a13829https://doaj.org/toc/1176-9114https://doaj.org/toc/1178-2013Liang-Zhong Lv,1 Chen-Qi Tong,1 Jia Yu,1 Min Han,2 Jian-Qing Gao21Department of Pharmacy, Zhejiang Provincial People's Hospital, Hangzhou, People's Republic of China; 2Institute of Pharmaceutics, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, People's Republic of ChinaAbstract: Hydroxysafflor yellow A (HSYA) is an effective ingredient of the Chinese herb Carthamus tinctorius L, which has high water solubility and low oral bioavailability. This research aims to develop a hydrophobic nanoparticle that can enhance the oral absorption of HSYA. Transmission electron microscopy and freeze-fracture replication transmission election microscopy showed that the HSYA nanoparticles have an irregular shape and a narrow size distribution. Zonula occludens 1 protein (ZO–1) labeling showed that the nanoparticles with different dilutions produced an opening in the tight junctions of Caco-2 cells without inducing cytotoxicity to the cells. Both enhanced uptake in Caco-2 cells monolayer and increased bioavailability in rats for HSYA nanoparticles indicated that the formulation could improve bioavailability of HSYA significantly after oral administration both in vitro and in vivo.Keywords: hydroxysafflor yellow A, nanoparticles, Caco-2 cells, bioavailability, absorptionLv LZTong CQYu JHan MGao JQDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2013, Iss default, Pp 2709-2717 (2013)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine (General) R5-920
spellingShingle	Medicine (General) R5-920 Lv LZ Tong CQ Yu J Han M Gao JQ Mechanism of enhanced oral absorption of hydrophilic drug incorporated in hydrophobic nanoparticles
description	Liang-Zhong Lv,1 Chen-Qi Tong,1 Jia Yu,1 Min Han,2 Jian-Qing Gao21Department of Pharmacy, Zhejiang Provincial People's Hospital, Hangzhou, People's Republic of China; 2Institute of Pharmaceutics, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, People's Republic of ChinaAbstract: Hydroxysafflor yellow A (HSYA) is an effective ingredient of the Chinese herb Carthamus tinctorius L, which has high water solubility and low oral bioavailability. This research aims to develop a hydrophobic nanoparticle that can enhance the oral absorption of HSYA. Transmission electron microscopy and freeze-fracture replication transmission election microscopy showed that the HSYA nanoparticles have an irregular shape and a narrow size distribution. Zonula occludens 1 protein (ZO–1) labeling showed that the nanoparticles with different dilutions produced an opening in the tight junctions of Caco-2 cells without inducing cytotoxicity to the cells. Both enhanced uptake in Caco-2 cells monolayer and increased bioavailability in rats for HSYA nanoparticles indicated that the formulation could improve bioavailability of HSYA significantly after oral administration both in vitro and in vivo.Keywords: hydroxysafflor yellow A, nanoparticles, Caco-2 cells, bioavailability, absorption
format	article
author	Lv LZ Tong CQ Yu J Han M Gao JQ
author_facet	Lv LZ Tong CQ Yu J Han M Gao JQ
author_sort	Lv LZ
title	Mechanism of enhanced oral absorption of hydrophilic drug incorporated in hydrophobic nanoparticles
title_short	Mechanism of enhanced oral absorption of hydrophilic drug incorporated in hydrophobic nanoparticles
title_full	Mechanism of enhanced oral absorption of hydrophilic drug incorporated in hydrophobic nanoparticles
title_fullStr	Mechanism of enhanced oral absorption of hydrophilic drug incorporated in hydrophobic nanoparticles
title_full_unstemmed	Mechanism of enhanced oral absorption of hydrophilic drug incorporated in hydrophobic nanoparticles
title_sort	mechanism of enhanced oral absorption of hydrophilic drug incorporated in hydrophobic nanoparticles
publisher	Dove Medical Press
publishDate	2013
url	https://doaj.org/article/86a3bfe23b1149639f00c4cceb064f52
work_keys_str_mv	AT lvlz mechanismofenhancedoralabsorptionofhydrophilicdrugincorporatedinhydrophobicnanoparticles AT tongcq mechanismofenhancedoralabsorptionofhydrophilicdrugincorporatedinhydrophobicnanoparticles AT yuj mechanismofenhancedoralabsorptionofhydrophilicdrugincorporatedinhydrophobicnanoparticles AT hanm mechanismofenhancedoralabsorptionofhydrophilicdrugincorporatedinhydrophobicnanoparticles AT gaojq mechanismofenhancedoralabsorptionofhydrophilicdrugincorporatedinhydrophobicnanoparticles
_version_	1718399524688363520

Mechanism of enhanced oral absorption of hydrophilic drug incorporated in hydrophobic nanoparticles

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