Since their advent in the early 1990s, nanomaterials hold promise to constitute improved technologies in the biomedical area. In particular, graphene quantum dots (GQDs) were conjectured to produce new or improve current methods used for bioimaging, drug delivery, and biomarker sensors for early detection of diseases. This review article critically compares and discusses current state-of-the-art use of GQDs in biology and health sciences. It shows the ability of GQDs to be easily functionalised for use as a targeted multimodal treatment and imaging platform. The in vitro and in vivo toxicity of GQDs are explored showing low toxicity for many types of GQDs.