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

Authors Lv L, Tong C, Yu j, Han M, Gao J

Received 30 April 2013

Accepted for publication 14 June 2013

Published 29 July 2013 Volume 2013:8(1) Pages 2709—2717


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Liang-Zhong Lv,1 Chen-Qi Tong,1 Jia Yu,1 Min Han,2 Jian-Qing Gao2

1Department 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 China

Abstract: 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

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