Novel norcantharidin-loaded liver targeting chitosan nanoparticles to enhance intestinal absorption
Yong-yan Bei1, Xiao-yan Chen1, Yang Liu1, Jing-yu Xu1, Wen-juan Wang1, Zong-lin Gu1, Kong-lang Xing1, Ai-jun Zhu1, Wei-liang Chen1, Lin-seng Shi1, Qin Wang1, Xue-nong Zhang1, Qiang Zhang21College of Pharmaceutical Science, Soochow University, Suzhou, 2Department of Pharmaceutics, School of Pharmaceu...
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Dove Medical Press
2012
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oai:doaj.org-article:e81f435b1ded44658ad09c6bca28174b2021-12-02T08:08:32ZNovel norcantharidin-loaded liver targeting chitosan nanoparticles to enhance intestinal absorption1176-91141178-2013https://doaj.org/article/e81f435b1ded44658ad09c6bca28174b2012-04-01T00:00:00Zhttp://www.dovepress.com/novel-norcantharidin-loaded-liver-targeting-chitosan-nanoparticles-to--a9625https://doaj.org/toc/1176-9114https://doaj.org/toc/1178-2013Yong-yan Bei1, Xiao-yan Chen1, Yang Liu1, Jing-yu Xu1, Wen-juan Wang1, Zong-lin Gu1, Kong-lang Xing1, Ai-jun Zhu1, Wei-liang Chen1, Lin-seng Shi1, Qin Wang1, Xue-nong Zhang1, Qiang Zhang21College of Pharmaceutical Science, Soochow University, Suzhou, 2Department of Pharmaceutics, School of Pharmaceutical Science, Peking University, Beijing, People's Republic of ChinaAbstract: In this paper, two novel liver-targeting nanoparticles, norcantharidin-loaded chitosan nanoparticles (NCTD-CS-NPs) and norcantharidin-associated galactosylated chitosan nanoparticles (NCTD-GC-NPs), were prepared using ionic cross-linkage. The physical properties, particle size, encapsulation efficiency, and drug release characteristics of the nanoparticles were investigated in vitro. To investigate the intestinal absorption mechanisms of the two preparations, a series of experiments was carried out, including in situ circulation method, in vitro everted gut sacs, and Ussing chamber perfusion technique. The absorption rate constants (Ka) of NCTD at different segments were found to be duodenum > jejunum > ileum > colon. The concentration had no distinctive effect on absorption kinetics, suggesting that drug absorption is not dose-dependent. The transport of NCTD was found to be inhibited by P-glycoprotein (P-gp) inhibitor, indicating that NCTD might be the substrate of P-gp. The order of the absorption enhancer effects were as follows: low molecular weight chitosan (CS-8kDa) . high molecular weight chitosan (CS-30kDa) > Poloxamer > sodium dodecyl sulfate (SDS) > sodium deoxycholate (SDCh). The results indicate that the chitosan nanoparticles can improve intestinal absorption of NCTD.Keywords: P-glycoprotein, absorption enhancersBei YYChen XYLiu YXu JYWang WJGu ZLXing KLZhu AJChen WLShi LSWang QZhang XNZhang QDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2012, Iss default, Pp 1819-1827 (2012) |
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Medicine (General) R5-920 Bei YY Chen XY Liu Y Xu JY Wang WJ Gu ZL Xing KL Zhu AJ Chen WL Shi LS Wang Q Zhang XN Zhang Q Novel norcantharidin-loaded liver targeting chitosan nanoparticles to enhance intestinal absorption |
description |
Yong-yan Bei1, Xiao-yan Chen1, Yang Liu1, Jing-yu Xu1, Wen-juan Wang1, Zong-lin Gu1, Kong-lang Xing1, Ai-jun Zhu1, Wei-liang Chen1, Lin-seng Shi1, Qin Wang1, Xue-nong Zhang1, Qiang Zhang21College of Pharmaceutical Science, Soochow University, Suzhou, 2Department of Pharmaceutics, School of Pharmaceutical Science, Peking University, Beijing, People's Republic of ChinaAbstract: In this paper, two novel liver-targeting nanoparticles, norcantharidin-loaded chitosan nanoparticles (NCTD-CS-NPs) and norcantharidin-associated galactosylated chitosan nanoparticles (NCTD-GC-NPs), were prepared using ionic cross-linkage. The physical properties, particle size, encapsulation efficiency, and drug release characteristics of the nanoparticles were investigated in vitro. To investigate the intestinal absorption mechanisms of the two preparations, a series of experiments was carried out, including in situ circulation method, in vitro everted gut sacs, and Ussing chamber perfusion technique. The absorption rate constants (Ka) of NCTD at different segments were found to be duodenum > jejunum > ileum > colon. The concentration had no distinctive effect on absorption kinetics, suggesting that drug absorption is not dose-dependent. The transport of NCTD was found to be inhibited by P-glycoprotein (P-gp) inhibitor, indicating that NCTD might be the substrate of P-gp. The order of the absorption enhancer effects were as follows: low molecular weight chitosan (CS-8kDa) . high molecular weight chitosan (CS-30kDa) > Poloxamer > sodium dodecyl sulfate (SDS) > sodium deoxycholate (SDCh). The results indicate that the chitosan nanoparticles can improve intestinal absorption of NCTD.Keywords: P-glycoprotein, absorption enhancers |
format |
article |
author |
Bei YY Chen XY Liu Y Xu JY Wang WJ Gu ZL Xing KL Zhu AJ Chen WL Shi LS Wang Q Zhang XN Zhang Q |
author_facet |
Bei YY Chen XY Liu Y Xu JY Wang WJ Gu ZL Xing KL Zhu AJ Chen WL Shi LS Wang Q Zhang XN Zhang Q |
author_sort |
Bei YY |
title |
Novel norcantharidin-loaded liver targeting chitosan nanoparticles to enhance intestinal absorption |
title_short |
Novel norcantharidin-loaded liver targeting chitosan nanoparticles to enhance intestinal absorption |
title_full |
Novel norcantharidin-loaded liver targeting chitosan nanoparticles to enhance intestinal absorption |
title_fullStr |
Novel norcantharidin-loaded liver targeting chitosan nanoparticles to enhance intestinal absorption |
title_full_unstemmed |
Novel norcantharidin-loaded liver targeting chitosan nanoparticles to enhance intestinal absorption |
title_sort |
novel norcantharidin-loaded liver targeting chitosan nanoparticles to enhance intestinal absorption |
publisher |
Dove Medical Press |
publishDate |
2012 |
url |
https://doaj.org/article/e81f435b1ded44658ad09c6bca28174b |
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