抗HER2抗体修饰的聚乙二醇化壳聚糖载基因纳米粒的制备与表征  

Preparation and Characterization of Anti-HER2-modified mPEG-Chitosan Nanoparticles

作　　者：王一伊[1] 刘培峰[2,3] 杜晶[1] 李凤华[1] 段友容[2,3] 

机构地区：[1]上海交通大学医学院附属仁济医院超声医学科,上海200127 [2]上海交通大学医学院附属仁济医院 [3]上海市肿瘤研究所,上海200032

出　　处：《中国医药工业杂志》2012年第11期927-931,共5页Chinese Journal of Pharmaceuticals

摘　　要：以甲氧基聚乙二醇(mPEG)接枝壳聚糖(CS)为载体制备载小干扰RNA(siRNA)的纳米粒,并用抗人表皮生长因子受体2抗体(anti-HER2)进行表面修饰。扫描电镜观察到所得纳米粒的形态为类球形,平均粒径为(160±2.4)nm,平均电位(23.5±1.7)mV,包封率为(64.2±1.6)%。体外释放试验表明,制品在初始12 h内(突释阶段)的累积释放率为14%～18%,144 h时累积释放率约70%。体外细胞试验表明,表面经anti-HER2修饰的纳米粒对SKBR-3乳腺癌细胞无明显毒性,提示其作为基因递送载体安全性较高、毒性较低。The nanoparticles loaded with small interfering RNA （siRNA） were prepared with monomethoxy polyethylene glycol （mPEG） grafted chitosan （CS） as the carrier and then surface modified with anti-human epidermal growth factor receptor 2 antibody （anti-HER2）. The observation of the scanning electron microscope showed that the product was spherical. The mean particle size, ~ potential and encapsulation efficiency of the product were （160±2.4） nm, （23.5±1.7） mV and （64.2±1.6） %, respectively. The results of in vitro release test showed that the burst release in the initial 12 h was 14% ± 18 % and the cumulative release at 144 h was about 70 %. The results of in vitro cytotoxicity test showed that the nanoparticles modified with anti-HER2 had no obvious toxicity to SKBR-3 breast cancer cells, which suggested that it might be developed as a potential gene delivery carrier with high security and low toxicity.

关 键 词：聚乙二醇接枝壳聚糖 小干扰RNA 抗人表皮生长因子受体2抗体 纳米粒 

分 类 号：R944.9[医药卫生—药剂学]