▎ 摘　　要

In this Review article, recent progress in matter of graphene oxide (GO) synthesis and its functionalization via a vast range of materials, including small molecules, polymers, and biomolecules, were reported and systematically summarized in order to overcome the inherent drawbacks of GO nanocarriers and thereby make these nanocarriers suitable for delivering chemotherapeutic agents, genes, and short interfering RNAs. Briefly, this work describes current strategies for the large scale production of GO and modification of graphene-based nanocarriers surfaces through practical chemical approaches, improving their biocompatibility and declining their toxicity. It also describes the most relevant cases of study suitable to demonstrate the role of graphene and graphene derivatives (GD) as nanocarrier for anti-cancer drugs and genes (e.g. miRNAs). Moreover, the controlled release mechanisms within the cell compartments and blood pH for targeted therapeutics release in the acidic environment of tumor cells or in intracellular compartments are mentioned and explored.