Implementing graphene quantum dots (GQDs) as zero-dimensional nanomaterials for drug delivery is obvious due to exceptional physicochemical, optical (photoluminescence and electrochemiluminescence), and biological properties such as good photostability, emission of multicolor, biocompatibility, less toxicity, and chemical inertness. Moreover, surface adhesion to organic molecules and planner structure increases surface area compared to volume, quantum confinement, and edge effects, facilitating drug delivery applications. Specific properties related to drug delivery of GQDs are emphasized at the beginning of this chapter. Several synthesis procedures of GQDs, including bottom-up and top-down methods with newly developed preparation of GQDs for drug delivery applications, are highlighted. Finally, this chapter will summarize novel applications in medication administration, stating limitations, challenges, and future scope of research.