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RGD-modified polymeric micelles as potential carriers for targeted delivery to integrin-overexpressing tumor vasculature and tumor cells
Wang, Yiguang; Wang, Xun; Zhang, Yifei; Yang, Shijin; Wang, Jiancheng; Zhang, Xuan; Zhang, Qiang
关键词Tumor vasculature tumor cells polymeric micelles integrin targeting
刊名JOURNAL OF DRUG TARGETING
2009-07-01
DOI10.1080/10611860902974085
17期:6页:459-467
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]STERICALLY STABILIZED LIPOSOMES ; IMPROVED ANTITUMOR EFFICACY ; BLOCK-COPOLYMER MICELLES ; IN-VIVO ; DRUG-DELIVERY ; INTRACELLULAR DELIVERY ; BREAST-CANCER ; DOXORUBICIN ; INTERNALIZATION ; NANOPARTICLES
英文摘要

Integrins alpha v beta 3 and alpha v beta 5 are overexpressed in angiogenic tumor endothelial cells and malignant tumor cells, making them attractive targets for cancer therapy. In this study, an integrin alpha v beta 3 and alpha v beta 5 binding tripeptide, RGD (Arg-Gly-Asp), was conjugated with the surface of poly(ethylene glycol)-block-poly(D,L-lactide) (PEG-PLA) micelles. A lipophilic fluorescent probe, Dil, was loaded into both the nontargeted methoxy PEG-PLA (mPEG-PLA) micelles and the targeted RGD-modified PEG-PLA micelles. The Dil-loaded targeted micelles had a size of 24.2 nm. The targeted micelles were stable in phosphate buffered saline and exhibited a negligible leakage in culture medium. Transmission electron microscopy analysis showed that targeted micelles were spherical in shape. Cell uptake of Dil-labeled targeted micelles by human umbilical vein endothelial cells and melanoma B16 cells was investigated by spectrophotofluorometry and confocal microscopy techniques. Results revealed that RGD-modified micelles significantly facilitated the intracellular delivery of the encapsulated agents via integrin-mediated endocytosis. This study suggests that RGD-modified PEG-PLA micelles are promising drug carriers for targeted delivery to both angiogenic tumor endothelial cells and tumor cells and that the targeted micelles may be attractive carriers for combination cancer therapy against both targets.

语种英语
WOS记录号WOS:000268243200006
引用统计
被引频次:34[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/400002259/62317
专题北京大学药学院
北京大学药学院_药剂学系
北京大学口腔医学院_中心实验室
作者单位Peking Univ, Sch Pharmaceut Sci, State Key Lab Nat & Biomimet Drugs, Beijing 100083, Peoples R China
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GB/T 7714
Wang, Yiguang,Wang, Xun,Zhang, Yifei,et al. RGD-modified polymeric micelles as potential carriers for targeted delivery to integrin-overexpressing tumor vasculature and tumor cells[J]. JOURNAL OF DRUG TARGETING,2009,17(6):459-467.
APA Wang, Yiguang.,Wang, Xun.,Zhang, Yifei.,Yang, Shijin.,Wang, Jiancheng.,...&Zhang, Qiang.(2009).RGD-modified polymeric micelles as potential carriers for targeted delivery to integrin-overexpressing tumor vasculature and tumor cells.JOURNAL OF DRUG TARGETING,17(6),459-467.
MLA Wang, Yiguang,et al."RGD-modified polymeric micelles as potential carriers for targeted delivery to integrin-overexpressing tumor vasculature and tumor cells".JOURNAL OF DRUG TARGETING 17.6(2009):459-467.
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