The rapid advancements in nanotechnology have paved the way for developing efficient and targeted drug delivery systems using nanomaterials. Among various nanomaterials, graphene-based nanocomposites have shown great potential for drug delivery applications owing to their unique physicochemical characteristics, including a substantial surface area, exceptional mechanical strength, and high electrical conductivity. This chapter in book aims to provide a comprehensive overview of the design, synthesis, and applications of graphene-based nanomaterials for drug delivery. The content is divided into six sub-topics, which collectively cover the essential aspects and recent advancements in the field.