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学科主题: 药学
题名:
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
作者: 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
发表日期: 2010-07-01
DOI: 10.1021/mp100033k
卷: 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
所属项目编号: 2009zx09310-001 ; 2009CB930300
项目资助者: National Development of Significant New Drugs ; National Basic Research Program of China
WOS记录号: WOS:000280448100026
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/65638
Appears in Collections:北京大学药学院_药剂学系_期刊论文

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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

Recommended Citation:
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.
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