Recent advancements in the development of graphene quantum dots (GQDs) in the field of nanomedicine are reviewed. Following an overview of the properties of GQDs, progress in top‐down and bottom‐up synthesis methods are presented. Application of GQDs in various modes of bioimaging, biosensing, and therapy are also discussed, with a subsequent discussion of future directions. Abstract Graphene quantum dots (GQDs) are carbon‐based, nanoscale particles that exhibit excellent chemical, physical, and biological properties that allow them to excel in a wide range of applications in nanomedicine. The unique electronic structure of GQDs confers functional attributes onto these nanomaterials such as strong and tunable photoluminescence for use in fluorescence bioimaging and biosensing, a high loading capacity of aromatic compounds for small‐molecule drug delivery, and the ability to absorb incident radiation for use in the cancer‐killing techniques of photothermal and photodynamic therapy. Recent advances in the development of GQDs as novel, multifunctional biomaterials are presented with a focus on their physicochemical, electronic, magnetic, and biological properties, along with a discussion of technical progress in the synthesis of GQDs. Progress toward the application of GQDs in bioimaging, biosensing, and therapy is reviewed, along with a discussion of the current limitations and future directions of this exciting material.

Published in: "Advanced Materials".