This book comprehensively reviews the incorporation of different types of carbon-based nanomaterials for application in targeted and controlled drug delivery systems. Carbon-based nanomaterials play a vital role as vectors and scaffolds during drug delivery owing to their ultra-small size, non-toxicity, and high water solubility. The chapters in this book present the use of different carbon-based nanomaterials (such as graphene, carbon quantum dots, carbon nanotubes, fullerenes, and carbon nanofibers) into polymeric and polysaccharide-based matrices for the designing of effective drug delivery vehicles which demonstrate superior performance compared to traditional drug delivery systems. In particular, it demonstrates the incorporation of carbon-based nanomaterials into supramolecular drug delivery systems leading to improved drug delivery properties. This book aims to be a reference for researchers and scientists interested in new nanomaterials for drug delivery applications.