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

Folic acid (FA)-gamma cyclodextrin (gamma CD)-C-60 was synthesized in this study as a carrier for tumor-targeted drug delivery to enhance the anticancer effect of carboplatin (CBP). FA-gamma CD and C-60-CBP were prepared and C-60-CBP was then entrapped into FA-gamma CD through host-guest effect. FA-gamma CD-C-60 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-gamma CD-C-60-CBP had more significant anticancer effects than CBP alone, showing no obvious toxic effects on zebrafish at concentration as high as 500 mu g/mL. These results suggest that FA-gamma CD-C-60 may provide an effective strategy for administration of antineoplastics, with great promise in future targeted therapy for cancers.