Folic Acid Functionalized γ-Cyclodextrin C₆₀, A Novel Vehicle for Tumor-Targeted Drug Delivery.

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.