Liu Yan, Pu Yunzhu, Sun Lan, Yao Hongjuan, Zhao Baoquan, Zhang Renzheng, Zhang Yingge
J Biomed Nanotechnol. 2016 Jul;12(7):1393-403. doi: 10.1166/jbn.2016.2275.
Folic acid (FA)-γ cyclodextrin (γ CD)-C60 was synthesized in this study as a carrier for tumor-targeted drug delivery to enhance the anticancer effect of carboplatin (CBP). FA-γ CD and C60-CBP were prepared and C60-CBP was then entrapped into FA-γ CD through host-guest effect. FA-γ CD-C60 significantly increased the intracellular uptake and release of CBP, thereby providing higher cytotoxicity against the HeLa cells with high expression of folate receptor (FR). In vivo experiments revealed that FA-γ CD-C60-CBP had more significant anticancer effects than CBP alone, showing no obvious toxic effects on zebrafish at concentration as high as 500 μg/mL. These results suggest that FA-γ CD-C60 may provide an effective strategy for administration of antineoplastics, with great promise in future targeted therapy for cancers.
本研究合成了叶酸（FA）-γ环糊精（γCD）-C60作为肿瘤靶向给药载体，以增强卡铂（CBP）的抗癌效果。制备了FA-γCD和C60-CBP，然后通过主客体效应将C60-CBP包封在FA-γCD中。FA-γCD-C60显著增加了CBP的细胞内摄取和释放，从而对叶酸受体（FR）高表达的HeLa细胞具有更高的细胞毒性。体内实验表明，FA-γCD-C60-CBP比单独使用CBP具有更显著的抗癌效果，在浓度高达500μg/mL时对斑马鱼无明显毒性作用。这些结果表明，FA-γCD-C60可能为抗肿瘤药物给药提供一种有效的策略，在未来癌症靶向治疗中具有广阔前景。
