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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Autores principales: 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
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Publicado: Dove Medical Press 2012
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Acceso en línea:https://doaj.org/article/e81f435b1ded44658ad09c6bca28174b
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spelling 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)
institution DOAJ
collection DOAJ
language EN
topic Medicine (General)
R5-920
spellingShingle 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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