Liu Peifeng, Wang Hongbin, Wang Qi, Sun Ying, Shen Ming, Zhu Mingjie, Wan Zhiyong, Duan Yourong
Shanghai Cancer Institute, Renji Hospital, Shanghai Jiao Tong University School of Medicine, Shanghai 200032, China.
J Nanosci Nanotechnol. 2012 Jun;12(6):4467-71. doi: 10.1166/jnn.2012.6213.
The main purpose of this study was to evaluate the targeting effect of cyclic arginine-glycine-aspartic peptide (cRGD)-modified monomethoxy (polyethylene glycol)-poly (D, L-lactide-co-glycolide)-poly (L-lysine) nanoparticles (mPEG-PLGA-PLL-cRGD NPs) for gastric cancer SGC-7901 cells. We prepared the 5-Fulorouracil (5Fu)-loaded mPEG-PLGA-PLL-cRGD (5Fu/mPEG-PLGA-PLL-cRGD) NPs that had an average particle size of 180 nm and a zeta potential 2.77 mV. The results of cytotoxicity demonstrated the mPEG-PLGA-PLL-cRGD NPs showed the ignorable cytotoxicity and the 5Fu/mPEG-PLGA-PLL-cRGD NPs could significantly enhance the cytotoxicity of 5Fu. In vitro drug release experiments showed that the release of drug was effectively prolonged and sustained. The results of confocal laser scanning microscope (CLSM) and flow cytometer analysis demonstrated that the fluorescence intensity of the SGC-7901 gastric cancer cells treated with Rb/mPEG-PLGA-PLL-cRGD NPs was significantly higher than that treated with Rb, this suggested that Rb/mPEG-PLGA-PLL-cRGD NPs could effectively be internalized by SGC-7901 gastric cancer cells. In summary, the above experimental results illustrate that mPEG-PLGA-PLL-cRGD NPs have great potential to be used as an effective delivery carriers.
本研究的主要目的是评估环精氨酸 - 甘氨酸 - 天冬氨酸肽（cRGD）修饰的单甲氧基（聚乙二醇）-聚（D，L-丙交酯 - 乙交酯）-聚（L-赖氨酸）纳米颗粒（mPEG-PLGA-PLL-cRGD NPs）对胃癌SGC-7901细胞的靶向作用。我们制备了负载5-氟尿嘧啶（5Fu）的mPEG-PLGA-PLL-cRGD（5Fu/mPEG-PLGA-PLL-cRGD）纳米颗粒，其平均粒径为180 nm，zeta电位为2.77 mV。细胞毒性结果表明，mPEG-PLGA-PLL-cRGD纳米颗粒显示出可忽略的细胞毒性，而5Fu/mPEG-PLGA-PLL-cRGD纳米颗粒可显著增强5Fu的细胞毒性。体外药物释放实验表明，药物释放得到有效延长和持续。共聚焦激光扫描显微镜（CLSM）和流式细胞仪分析结果表明，用Rb/mPEG-PLGA-PLL-cRGD纳米颗粒处理的SGC-7901胃癌细胞的荧光强度明显高于用Rb处理的细胞，这表明Rb/mPEG-PLGA-PLL-cRGD纳米颗粒可被SGC-7901胃癌细胞有效内化。综上所述，上述实验结果表明mPEG-PLGA-PLL-cRGD纳米颗粒有很大潜力用作有效的递送载体。
