期刊
ACTA BIOMATERIALIA
卷 23, 期 -, 页码 127-135出版社
ELSEVIER SCI LTD
DOI: 10.1016/j.actbio.2015.05.021
关键词
Poly(2-ethyl-2-oxazoline)-poly(D,L-lactide); pH-responsive polymeric micelles; Paclitaxel; Integrin alpha(v)beta(3); Tumor-targeting
资金
- National Natural Science Foundation of China [81172990]
- National Key Science Research Program of China (973 Program) [2015CB932100]
- Innovation Team of Ministry of Education [BMU20110263]
Cyclic RGDyK (cRGDyK)-conjugated pH-sensitive polymeric micelles were fabricated for targeted delivery of paclitaxel to prostate cancer cells based on pH-sensitive copolymer poly(2-ethyl-2-oxazoline)-poly(D,L-lactide) (PEOz-PLA) and cRGDyK-PEOz-PLA to enhance antitumor efficacy. The prepared micelles with an average diameter of about 28 nm exhibited rapid release behavior at endo/lysosome pH, effectively enhanced the cytotoxicity of paclitaxel to PC-3 cells by increasing the cellular uptake, which was correlated with integrin alpha(v)beta(3) expression in tumor cells. The active targeting activity of the micelles was further confirmed by in vivo real time near-infrared fluorescence imaging in PC-3 tumor-bearing nude mice. Moreover, the active targeting and pH-sensitivity endowed cRGDyK-conjugated micelles with a higher antitumor effect in PC-3 xenograft-bearing nude mice compared with unmodified micelles and Taxol with negligible systemic toxicity. Therefore, these results suggested that cRGDyK-conjugated pH-sensitive polymeric micelles may be a promising delivery system for efficient delivery of anticancer drugs to treat integrin alpha(v)beta(3)-rich prostate cancers. (C) 2015 Acta Materialia Inc. Published by Elsevier Ltd. All rights reserved.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据