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Cyclosporin A-Loaded Poly(ethylene glycol)-b-poly(D,L-lactic acid) Micelles: Preparation, in Vitro and in Vivo Characterization and Transport Mechanism across the Intestinal Barrier
Zhang, Yanhui1; Li, Xinru1; Zhou, Yanxia1; Fan, Yating1; Wang, Xiaoning1; Huang, Yanqing2; Liu, Yan1
关键词Cyclosporin A monomethoxy poly(ethylene glycol)-b-poly(D,L-lactic acid) polymeric micelles oral administration Caco-2 cells transport mechanism P-glycoprotein
刊名MOLECULAR PHARMACEUTICS
2010-07-01
DOI10.1021/mp100033k
7期:4页:1169-1182
收录类别SCI
文章类型Article
WOS标题词Science & Technology
类目[WOS]Medicine, Research & Experimental ; Pharmacology & Pharmacy
研究领域[WOS]Research & Experimental Medicine ; Pharmacology & Pharmacy
关键词[WOS]WATER-SOLUBLE DRUGS ; P-GLYCOPROTEIN EFFLUX ; AMPHIPHILIC DIBLOCK COPOLYMERS ; PLURONIC BLOCK-COPOLYMERS ; POLYMERIC MICELLES ; CACO-2 CELLS ; ORAL DELIVERY ; RELEASE BEHAVIORS ; SENSITIVE NANOPARTICLES ; MEMBRANE FLUIDIZATION
英文摘要

To improve the oral bioavailability of poorly water-soluble cyclosporin A (CyA), polymeric micelles based on monomethoxy poly(ethylene glycol)-b-poly(D,L-lactic acid) (mPEG-PLA) were prepared. In vitro release test showed that the cumulative release percentage, about 85%, of CyA from polymeric micelles within 24 h was comparable to that from Sandimmun Neoral, the currently available oral formulation of CyA. A relative oral bioavailability of 137% in rats compared with Sandimmun Neoral was demonstrated for CyA-loaded polymeric micelles. The other aim of the current work was to study the transport mechanism of mPEG-PLA micelles across the intestinal barrier. It was found that polymeric micelles could significantly increase the permeability of CyA across Caco-2 monolayers without significantly affecting transepithelial electrical resistance values, and the apparent permeation coefficient (P(app)) of CyA was significantly higher in the AP-BL direction compared to that in the BL-AP direction, suggesting that polymeric micelles might undergo an active AP to BL transport that probably involved endocytosis which was confirmed by confocal microscope observation. The permeation of CyA through Caco-2 monolayers showed that the P(app) was significantly increased when CyA was formulated with the copolymer below its critical association concentration (CAC) and no significant difference was found above its CAC, implying that mPEG-PLA monomers affected the intestinal P-gp efflux pumps. Therefore, the mPEG-PLA micelles seemed to be a good candidate for oral delivery of poorly soluble drugs.

语种英语
WOS记录号WOS:000280448100026
项目编号2009zx09310-001 ; 2009CB930300
资助机构National Development of Significant New Drugs ; National Basic Research Program of China
引用统计
被引频次:25[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/65638
专题北京大学药学院_药剂学系
作者单位1.Peking Univ, Dept Pharmaceut, Sch Pharmaceut Sci, Beijing 100191, Peoples R China
2.Peking Univ, Pharmaceut Teaching Expt Ctr, Sch Pharmaceut Sci, Beijing 100191, Peoples R China
推荐引用方式
GB/T 7714
Zhang, Yanhui,Li, Xinru,Zhou, Yanxia,et al. Cyclosporin A-Loaded Poly(ethylene glycol)-b-poly(D,L-lactic acid) Micelles: Preparation, in Vitro and in Vivo Characterization and Transport Mechanism across the Intestinal Barrier[J]. MOLECULAR PHARMACEUTICS,2010,7(4):1169-1182.
APA Zhang, Yanhui.,Li, Xinru.,Zhou, Yanxia.,Fan, Yating.,Wang, Xiaoning.,...&Liu, Yan.(2010).Cyclosporin A-Loaded Poly(ethylene glycol)-b-poly(D,L-lactic acid) Micelles: Preparation, in Vitro and in Vivo Characterization and Transport Mechanism across the Intestinal Barrier.MOLECULAR PHARMACEUTICS,7(4),1169-1182.
MLA Zhang, Yanhui,et al."Cyclosporin A-Loaded Poly(ethylene glycol)-b-poly(D,L-lactic acid) Micelles: Preparation, in Vitro and in Vivo Characterization and Transport Mechanism across the Intestinal Barrier".MOLECULAR PHARMACEUTICS 7.4(2010):1169-1182.
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