▎ 摘　　要

An efficient and biocompatible drug nanocarrier is essential for nanomedicines to realize their full therapeutic potential. Here, we investigate the loading of a selective and potent anticancer drug, beta-lapachone (beta-lap), on a magnetite nanoparticle-decorated reduced graphene oxide (Fe3O4/rGO) and the in vitro anticancer efficacy of beta-lap loaded Fe3O4/rGO. Reduced graphene oxide (rGO) with magnetic functionality was prepared via electrostatic interaction between positively charged magnetite (Fe3O4) nanoparticles and negatively charged GO, followed by hydrazine reduction of GO to rGO. The prepared Fe3O4/rGO shows that Fe3O4 makes the Fe3O4/rGO hybrid magnetically separable for easy handling during drug loading and release and the Fe3O4/rGO hybrid exhibits significantly higher loading capacity than that of Fe3O4/GO, suggesting that restoration of the graphene basal plane upon reduction of GO enhances the interaction between beta-lap and rGO. Cellular uptake studies using fluorescently labeled Fe3O4/rGO verifies successful internalization of Fe3O4/rGO into the cytoplasm while rGO without hybridized Fe3O4 has poor uptake performance. Furthermore, beta-lap loaded Fe3O4/rGO shows remarkably high cytotoxicity toward MCF-7 breast cancer cells while the blank Fe3O4/rGO produces no cytotoxic effects. The cytotoxicity results suggest that Fe3O4/rGO is an efficient drug carrier for anticancer treatments. The fine-tuning of the chemical structures of graphene oxides by reduction chemistry may provide a universal route for controlled loading and release of drugs or biomolecules to construct advanced delivery vehicles.