The carbon-based nanomaterials are promising candidates in the field of drug delivery. Their unique physicochemical properties and remarkable biocompatibility are garnering major interest for their application in drug delivery. This chapter delivers a comprehensive overview of the past, present, and future directions of utilizing carbon-based nanomaterials for drug delivery and other biomedical applications. The chapter discusses in detail about drug delivery by nanomaterials based on graphene, graphene quantum dots (GQDs), carbon nanotubes (CNTs), carbon nanodiamonds (NDs), carbon nano-onions (CNOs), carbon nanohorns (CNHs), and fullerene. Through this comprehensive examination of the past, present, and future of carbon-based nanomaterials for drug delivery, the chapter aims to provide valuable insights to researchers, scientists, and clinicians involved in developing next-generation drug delivery systems with enhanced efficacy and reduced adverse effects.