The integration of carbon nanomaterials in supramolecular architectures has demonstrated potential as a viable approach for drug delivery, and this chapter presents a concise overview of this prospect. Because of their one-of-a-kind physicochemical features, carbon nanostructures are being eyed as potential medication delivery devices. To enhance pharmaceuticals’ solubility, stability, and bioavailability, supramolecular chemistry enables synthesizing complex structures with distinctive characteristics and activities. The chapter examines the fundamental principles underlying supramolecular chemistry, an exploration of the characteristics and implementation of carbon nanomaterials, and a comprehensive analysis of the benefits and constraints associated with their use in drug administration. Examples of carbon nanomaterial-incorporated supramolecular drug delivery systems are presented, and the future directions and potential applications of this approach are discussed. In conclusion, this chapter emphasizes the promise of carbon nanomaterial as an efficient and effective supramolecular drug delivery technology with various therapeutic applications.