 Abstract this review focuses on the recent advances in the synthesis of graphene quantum dots, GQDs, and their applications in drug delivery. To give a brief understanding about the preparation of GQDs, recent advances in methods of GQD synthesis are first presented. Afterwards, various drug delivery release modes of GQDS-based drug delivery systems such as EPR-PH delivery release mode, Ligand-PH delivery release mode, EPR photothermal delivery release mode, and core-shell photothermal magnetic thermal delivery release mode are reviewed. Finally, the current challenges and the prospective application of GQDs in drug delivery are discussed. This article was authored by Chan Hong-Jiao, Xue Bin Song, Wei Liu, and others.