Novel norcantharidin-loaded liver targeting chitosan nanoparticles to enhance intestinal absorption
| Autor: | Qin Wang, Qiang Zhang, Wei-liang Chen, Xiao-yan Chen, Kong-lang Xing, Yong-Yan Bei, Jing-Yu Xu, Aijun Zhu, Zong-lin Gu, Wen-Juan Wang, Yang Liu, Lin-seng Shi, Xue-nong Zhang |
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| Jazyk: | angličtina |
| Rok vydání: | 2012 |
| Předmět: |
Male
Absorption (pharmacology) Materials science Biophysics Pharmaceutical Science Bioengineering P-glycoprotein In Vitro Techniques Intestinal absorption Rats Sprague-Dawley Biomaterials Chitosan chemistry.chemical_compound Drug Delivery Systems Microscopy Electron Transmission International Journal of Nanomedicine Drug Discovery Animals Organic chemistry ATP Binding Cassette Transporter Subfamily B Member 1 Sodium dodecyl sulfate Original Research Drug Carriers Norcantharidin Ussing chamber Organic Chemistry absorption enhancers General Medicine Poloxamer Bridged Bicyclo Compounds Heterocyclic Antineoplastic Agents Phytogenic Rats Nanomedicine Intestinal Absorption Liver chemistry Nanoparticles Drug carrier Nuclear chemistry |
| Zdroj: | International Journal of Nanomedicine |
| ISSN: | 1178-2013 |
| Popis: | 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 |
| Databáze: | OpenAIRE |
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