羧甲基壳聚糖修饰阿霉素纳米脂质体的制备及体外细胞实验

Preparation of pH-Sensitive Doxorubicin Liposomes Modified with Carboxymethyl Chitosan and in Vitro Cell Research

以羧甲基壳聚糖(CMCT)为修饰剂,采用薄膜-pH梯度法制备具有pH敏感性的阿霉素纳米脂质体(CMCT-DOX-NL),以增加抗癌药物在肿瘤部位的蓄积,同时增强抗癌药物向肿瘤细胞内的传递。结果表明:制备的CMCT-DOX-NL粒子形貌圆整,粒径分布均匀为(38±22.1)nm,药物包封率为88.83%;相比传统的阿霉素纳米脂质体(DOX-NL),CMCT-DOX-NL与Hela细胞的结合和摄取均有所提高,对细胞的杀伤作用更强;CMCT-DOX-NL的体外药物释放具有明显的pH敏感性,比普通的阿霉素脂质体更能促进阿霉素(DOX)向肿瘤细胞内的传递。

To enhance the accumulation in the tumor and intracellular delivery of the encapsulated doxorubicin（DOX）,a pH-sensitive doxorubicin nanoliposomes（DOX-NL） modified with carboxymethyl chitosan（CMCT） was prepared by thin-film pH gradient.The nanoliposomes modified with CMCT showed good shape with an average particle size of（38±22.1） nm and the drug encapsulation efficiency was about 88.83%.The drug release of the CMCT-modified DOX nanoliposomes in vitro showed obvious pH sensitivity.The Hela cells treated with CMCT-DOX-NL showed remarkable increase in cellular association or DOX uptake compared with DOX-NL.The cytotoxicity of CMCT-DOX-NL on Hela cells was higher than that of DOX-NL.The pH-sensitive CMCT-modified DOX nanoliposomes promoted the delivery of the encapsulated DOX into the tumor cells.