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学科主题: 药学
题名:
Nanoscaled Polyion Complex Micelles for Targeted Delivery of Recombinant Hirudin to Platelets Based on Cationic Copolymer
作者: Wang, Fei1; Li, Xinru1; Zhou, Yanxia1; Zhang, Yanhui1; Chen, Xingwei1; Yang, Jingxiong1; Huang, Yanqing2; Liu, Yan1
关键词: Recombinant hirudin ; polyion complex micelles ; platelet-targeted ; poly(ethylene glycol)-grafted-chitosan ; anticoagulant activity ; inhibition of platelet aggregation
刊名: MOLECULAR PHARMACEUTICS
发表日期: 2010-05-01
DOI: 10.1021/mp900271r
卷: 7, 期:3, 页:718-726
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]: IN-VIVO CHARACTERIZATION ; PEG-GRAFTED CHITOSAN ; BLOCK-COPOLYMER ; CAPILLARY-ELECTROPHORESIS ; CONTROLLED-RELEASE ; DRUG-DELIVERY ; THROMBIN ; HEPARIN ; VITRO ; CORE
英文摘要:

Polyion complex (PIC) micelles based on methoxy poly(ethylene glycol)-grafted-chitosan (mPEG-g-chitosan) and Arg-Gly-Asp conjugated poly(ethylene glycol)-grafted-chitosan (RGD-PEG-g-chitosan) were designed as carriers for platelet-targeted delivery of recombinant hirudin variant-2 (rHV2). The rHV2-loaded plain PIC micelles (mPIC micelles) and RGD conjugated PIC micelles (RGD-PIC micelles) were successfully prepared with mean size of 30.9 +/- 0.5 nm and 41.9 +/- 1.8 nm, and their encapsulation efficiencies were 76.90 +/- 0.84% and 81.08 +/- 0.85%, respectively. The pharmacokinetics experiments showed that the mean retention time (MRT) of rHV2 encapsulated in both kinds of micelles was significantly prolonged, especially for mPIC micelles. The confocal laser scanning microscopy intuitively proved the specific binding of RGD-PIC micelles to platelets. The efficacies of rHV2-loaded RGD-PIC micelles were greatly better than those of rHV2-loaded mPIC micelles and rHV2 solution in aspect of anticoagulation and inhibition of platelet aggregation. These results suggested platelet-targeting specificity of RGD-PIC micelles and that RGD PIC micelles could potentially be used as a carrier for platelet-targeted delivery and long circulation of rHV2.

语种: 英语
所属项目编号: 2009zx09310-001 ; 2009CB930300
项目资助者: National Development of Significant New Drugs (New Preparation and New Technology ; National Basic Research Program of China
WOS记录号: WOS:000278452100010
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/54555
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 Lab Ctr, Beijing 100191, Peoples R China

Recommended Citation:
Wang, Fei,Li, Xinru,Zhou, Yanxia,et al. Nanoscaled Polyion Complex Micelles for Targeted Delivery of Recombinant Hirudin to Platelets Based on Cationic Copolymer[J]. MOLECULAR PHARMACEUTICS,2010,7(3):718-726.
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