NGR配体修饰的紫杉醇PEG-PLGA胶束抗肿瘤作用的体外体内研究(英文)

本研究制备了NGR(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(HT1080)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。

Anti-tumor efficiency of NGR-modified PEG-PLGA micelles containing paclitaxel:in vitro and in vivo

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 HT1080 tumor-bearing mice in vivo.