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学科主题: 药学
题名:
The antiangiogenic efficacy of NGR-modified PEG-DSPE micelles containing paclitaxel (NGR-M-PTX) for the treatment of glioma in rats
作者: Zhao, Bo-Jun1; Ke, Xi-Yu1; Huang, Yue1; Chen, Xiao-Mei1; Zhao, Xin1; Zhao, Bing-Xiang1; Lu, Wan-liang1,2; Lou, Jin-Ning3; Zhang, Xuan1; Zhang, Qiang1,2
关键词: Aminopeptidase N (APN) ; Asn-Gly-Arg (NGR) ; paclitaxel (PTX) ; DSPE-PEG micelles ; brain glioma-bearing rats ; antitumor efficacy
刊名: JOURNAL OF DRUG TARGETING
发表日期: 2011-06-01
DOI: 10.3109/1061186X.2010.504267
卷: 19, 期:5, 页:382-390
收录类别: SCI
文章类型: Article
WOS标题词: Science & Technology
类目[WOS]: Pharmacology & Pharmacy
研究领域[WOS]: Pharmacology & Pharmacy
关键词[WOS]: CATIONIC LIPOSOMES ; AMINOPEPTIDASE-N ; FIGHTING CANCER ; BRAIN-TUMORS ; MOUSE MODEL ; IN-VITRO ; CHEMOTHERAPY ; BINDING ; CELLS ; ANGIOGENESIS
英文摘要:

Aminopeptidase N (APN), recognized by Asn-Gly-Arg (NGR) peptides, is expressed in the pericytes associated with the BBB, and the main objective of this study is to confirm the hypothesis that NGR-modified DSPE-PEG micelles containing paclitaxel (NGR-M-PTX) can bind to and kill brain tumor angiogenic blood vessels and penetrate into the brain tumor interstitial space, resulting in direct cell death. NGR-M-PTX is prepared by a thin-film hydration method. The in vitro targeting characteristics of NGR-modified micelles on BMEC (murine brain microvascular endothelial cells) were investigated. The effect of NGR-M-PTX on BMEC proliferation and the cytotoxicity of NGR-M-PTX in C6 glioma cells were also tested. The antitumor activity NGR-M-PTX was evaluated in C6 glioma tumor-bearing rats in vivo. The particle size of NGR-M-PTX was approximately 54.2 nm. The drug encapsulation efficiency of NGR-M-PTX was 82.11 +/- 2.82%. The cellular coumarin-6 level of NGR-M-coumarin-6 in the BMEC was about 2.2-fold higher than that of M-coumarin-6. BMEC proliferation was significantly inhibited by NGR-M-PTX. NGR-M-PTX had a much lower IC(50) value than M-PTX and free drug. The growth of C6 glioma tumor was markedly inhibited by NGR-M-PTX compared with Taxol. In conclusion, our results show that antiangiogenic therapy using NGR-M-PTX exhibits potent in vivo antitumor activity in a C6 glioma-bearing animal model.

语种: 英语
所属项目编号: 30873170 ; 2007CB935800 ; 2009CB930300
项目资助者: National Natural Science Foundation of China ; National Basic Research Program of China (973 Program)
WOS记录号: WOS:000289995200008
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/67418
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, Sch Pharmaceut Sci, Dept Pharmaceut, Beijing 100191, Peoples R China
2.Peking Univ, Sch Pharmaceut Sci, State Key Lab Nat & Biomimet Drugs, Beijing 100191, Peoples R China
3.China Japan Friendship Hosp, Minist Hlth, Inst Clin Med Sci, Beijing 100029, Peoples R China

Recommended Citation:
Zhao, Bo-Jun,Ke, Xi-Yu,Huang, Yue,et al. The antiangiogenic efficacy of NGR-modified PEG-DSPE micelles containing paclitaxel (NGR-M-PTX) for the treatment of glioma in rats[J]. JOURNAL OF DRUG TARGETING,2011,19(5):382-390.
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