Zhang Xiaoke, Meng Lingjie, Lu Qinghua, Fei Zhaofu, Dyson Paul J
Department of Polymer Science and Engineering, School of Chemistry and Chemical Technology, Shanghai Jiao Tong University, Shanghai, PR China.
Biomaterials. 2009 Oct;30(30):6041-7. doi: 10.1016/j.biomaterials.2009.07.025. Epub 2009 Jul 29.
A targeted drug delivery system that is triggered by changes in pH based on single wall carbon nanotubes (SWCNTs), derivatized with carboxylate groups and coated with a polysaccharide material, can be loaded with the anticancer drug doxorubicin (DOX). The drug binds at physiological pH (pH 7.4) and is only released at a lower pH, for example, lysosomal pH and the pH characteristic of certain tumor environments. By manipulating the surface potentials of the modified nanotubes through modification of the polysaccharide coating, both the loading efficiency and release rate of the associated DOX can be controlled. Folic acid (FA), a targeting agent for many tumors, can be additionally tethered to the SWCNTs to selectively deliver DOX into the lysosomes of HeLa cells with much higher efficiency than free DOX. The DOX released from the modified nanotubes has been shown to damage nuclear DNA and inhibit the cell proliferation.
一种基于单壁碳纳米管（SWCNTs）的pH响应型靶向给药系统，该碳纳米管经羧基衍生化并包覆多糖材料，可负载抗癌药物阿霉素（DOX）。药物在生理pH值（pH 7.4）下结合，仅在较低pH值下释放，例如溶酶体pH值以及某些肿瘤环境的特征pH值。通过修饰多糖涂层来调控修饰纳米管的表面电位，可控制相关阿霉素的负载效率和释放速率。叶酸（FA）是许多肿瘤的靶向剂，可额外连接到单壁碳纳米管上，以比游离阿霉素更高的效率将阿霉素选择性地递送至HeLa细胞的溶酶体中。已证明从修饰纳米管释放的阿霉素会破坏核DNA并抑制细胞增殖。
