This review represent an overview of the graphene quantum dots synthesis and their application as carriers or probes for sensor, imaging, drug delivery and diagnosing of diseases. More specifically, recent advances in the integration of QDs with drug formulations for therapy and their potential toxicity in vitro and in vivo are highlighted. The current findings and challenges for optimizing QD/drug formulations with respect to optimal size and stability, short-term and long-term toxicity, and in vivo applications are described.