Zhang Huijuan, Chen Chengqun, Hou Lin, Jin Nan, Shi Jinjin, Wang Zhuo, Liu Yu, Feng Qianhua, Zhang Zhenzhong
a School of Pharmaceutical Sciences, Zhengzhou University , 100 Kexue Avenue, Zhengzhou, 450001, P.R. China.
J Drug Target. 2013 Apr;21(3):312-319. doi: 10.3109/1061186X.2012.749880.
A targeting and photothermal drug delivery system of doxorubicin (DOX) was successfully developed based on the AS1411 aptamer modified single wall carbon nanotubes (SWNTs). In this study, DOX was efficiently loaded onto SWNTs (DOX-AS1411-SWNTs) with drug loading of 121% and released from DOX-AS1411-SWNTs in a pH-dependent manner. Internalization analysis demonstrated that the tertiary complex (DOX-AS1411-SWNTs) could transfer into the cell through the AS1411-mediated endocytosis in 2 h. Moreover, the cytotoxicity test of DOX-AS1411-SWNTs showed higher inhibition effect on EC-109 cells compared to DOX control group. Meanwhile, 808 nm near-infrared laser was used here for photothermal treatment, and AS1411-SWNTs were proved to have a strong efficacy on tumor hyperthermia. Furthermore, with a focus on the G2-M phase, we found DOX-AS1411-SWNTs capable of altering G2-M cell-cycle phase, owing to the hyperthermia and synergistic effect.
基于AS1411适配体修饰的单壁碳纳米管（SWNTs）成功开发了一种阿霉素（DOX）靶向光热药物递送系统。在本研究中，DOX被高效负载到SWNTs上（DOX-AS1411-SWNTs），载药量为121%，且DOX-AS1411-SWNTs以pH依赖的方式释放。内化分析表明，三元复合物（DOX-AS1411-SWNTs）可在2小时内通过AS1411介导的内吞作用转运进入细胞。此外，DOX-AS1411-SWNTs的细胞毒性试验显示，与DOX对照组相比，其对EC-109细胞具有更高的抑制作用。同时，此处使用808nm近红外激光进行光热治疗，结果证明AS1411-SWNTs对肿瘤热疗具有很强的疗效。此外，聚焦于G2-M期，我们发现由于热疗和协同效应，DOX-AS1411-SWNTs能够改变G2-M细胞周期阶段。
