中文摘要：

本研究制备TNGR（asparagine—glycine—arginine）配体修饰的紫杉醇PEG-PLGA胶束（NGR-PM—PTX），并对其靶向肿瘤新生血管内皮细胞及肿瘤细胞所表达的氨肽酶N进行了研究。采用薄膜法制备NGR—PM．PTX胶束。通过针对人脐静脉内皮细胞（HUVEC），人纤维肉瘤细胞（HTl080）和人乳腺癌细胞（MCF－7）的流式细胞试验和激光共聚焦实验，在体外细胞水平上研究并证实了NGR配体修饰的聚合物胶束对于上述细胞的靶向效果。HT1080荷瘤裸鼠的体内药效学研究结果进一步证实NGR-PM-PTX的抗肿瘤药效。

英文摘要：

In the present study, we prepared novel NGR-modified PEG-PLGA polymeric micelles containing paclitaxel （NGR- PM-PTX） in order to evaluate their potential targeting to aminopeptidase N receptors expressed on tumor endothelial cells and the tumor cell surface and its anti-tumor activity in vitro and in vivo. NGR-PM-PTX was prepared by thin-film hydration method. The in vitro targeting characteristics of NGR-modified PM on HUVEC （human umbilical vein endothelial cells）, HT1080 （human fibrosarcoma cells） and MCF-7 （human breast adenocarcinoma cells） were then investigated. The anti-tumor activity of NGR-PM-PTX was evaluated in HT1080 tumor-bearing mice in vivo. The targeting activity of the NGR-modified PM was demonstrated by flow cytometry and confocal microscopy in vitro. NGR-PM-PTX also produced marked anti-tumor activity to HTI080 tumor-beating mice in vivo.