学科主题 | 药学 |
NGR-modified micelles enhance their interaction with CD13-overexpressing tumor and endothelial cells | |
Wang, Xun; Wang, Yiguang; Chen, Xiaomei; Wang, Jiancheng; Zhang, Xuan; Zhang, Qiang | |
关键词 | NGR CD13 Docetaxel Polymeric micelles CD13-overexpressing tumor |
刊名 | JOURNAL OF CONTROLLED RELEASE
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2009-10-01 | |
DOI | 10.1016/j.jconrel.2009.05.030 |
卷 | 139期:1页:56-62 |
收录类别 | SCI |
文章类型 | Article |
WOS标题词 | Science & Technology |
类目[WOS] | Chemistry, Multidisciplinary ; Pharmacology & Pharmacy |
资助者 | National Basic Research Program of China ; 863 Project ; National Basic Research Program of China ; 863 Project |
研究领域[WOS] | Chemistry ; Pharmacology & Pharmacy |
关键词[WOS] | AMINOPEPTIDASE-N ; POLYMERIC MICELLES ; DRUG-DELIVERY ; PEPTIDES ; CHEMOTHERAPY ; DOCETAXEL ; BINDING ; CANCER ; FORMULATION ; PACLITAXEL |
英文摘要 | Certain tumor cells and most tumor endothelial cells overexpress a membrane-spanning molecule, aminopeptidase N (CD13) isoform, which is the receptor for peptides containing the Asn-Gly-Arg (NGR) motif. NGR-modified docetaxel (DTX)-loaded PEG-b-PLA polymeric micelles (NGR-PM-DTX) were firstly developed and tested in vitro and in vivo, while DTX-loaded polymeric micelles (PM-DTX) and free DTX were used as controls. The NGR-PM-DTX containing DTX were about 35 nm in diameter with spherical shape and high encapsulation efficiency. It was demonstrated quantitatively by the spectrophotofluorometry and qualitatively by the confocal image analysis that NGR facilitates the uptake of micelles by CD13-overexpressed tumor cells (fibrosarcoma, HT1080) and endothelial cells (human umbilical vein endothelial cells. HUVEC). Free NGR inhibited cellular uptake of NGR-PM-DTX, revealing the mechanism of receptor-mediated endocytosis. Higher cytotoxicity, toward HT1080 cells and more efficient inhibition of HUVEC proliferation were also observed in NGR-PM-DTX groups, which were consistent well with the observation of cellular uptake. In BALB/c mice bearing HT1080 tumor xenografts, stronger antitumor efficacy and less body weight changes were shown in NGR-PM-DTX group, with good correlation between in vitro and in vivo. Therefore, it was concluded that NGR-PM could be a potential vehicle for delivering hydrophobic chemotherapeutic agents to CD13-overexpressing tumors. (C) 2009 Elsevier B.V. All rights reserved. |
语种 | 英语 |
所属项目编号 | 2009CB930300 ; 2007AA021811 |
资助者 | National Basic Research Program of China ; 863 Project ; National Basic Research Program of China ; 863 Project |
WOS记录号 | WOS:000270115800009 |
Citation statistics | |
文献类型 | 期刊论文 |
条目标识符 | http://ir.bjmu.edu.cn/handle/400002259/62396 |
Collection | 北京大学药学院 |
作者单位 | Peking Univ, Sch Pharmaceut Sci, State Key Lab Nat & Biomimet Drugs, Beijing 100191, Peoples R China |
Recommended Citation GB/T 7714 | Wang, Xun,Wang, Yiguang,Chen, Xiaomei,et al. NGR-modified micelles enhance their interaction with CD13-overexpressing tumor and endothelial cells[J]. JOURNAL OF CONTROLLED RELEASE,2009,139(1):56-62. |
APA | Wang, Xun,Wang, Yiguang,Chen, Xiaomei,Wang, Jiancheng,Zhang, Xuan,&Zhang, Qiang.(2009).NGR-modified micelles enhance their interaction with CD13-overexpressing tumor and endothelial cells.JOURNAL OF CONTROLLED RELEASE,139(1),56-62. |
MLA | Wang, Xun,et al."NGR-modified micelles enhance their interaction with CD13-overexpressing tumor and endothelial cells".JOURNAL OF CONTROLLED RELEASE 139.1(2009):56-62. |
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