▎ 摘　　要

Among various nanomaterials, graphene and its derivatives have attracted considerable research interest in diverse application areas-including nanomedicine-because of their extraordinary physical, chemical, and optical properties. Intensive research is underway to investigate the biomedical application of graphene and graphene based nanosystems as drug-delivery vehicles for cancer therapy, and this is considered as one of the novel therapeutic approaches for performing on-demand chemotherapy coupled with photothermal therapy or photodynamic therapy. Here, we systematically summarize recent progress in the synthesis and functionalization of graphene by using a vast range of materials, including small molecules, polymers, and biomolecules, in order to overcome the inherent drawbacks of graphene oxide (GO) nanocarriers and thereby make these nanocarriers suitable for delivering chemotherapeutic agents, genes, and short interfering RNAs. Moreover, we address the opportunities and challenges associated with future clinical application of GO for cancer therapy.