The design and synthesis of drug delivery systems (DDSs) with controlled release of pharmaceutical agents is essential to improve the treatment of cancer patients. So far, various types of DDSs encompassing nanomaterial scaffolds in combinations with organic, inorganic, and polymeric materials have been commercialized. In this field, chitosan and chitosan-modified polymers are the most considered natural biomaterials thank to their unique properties such as low cost, high viscosity, excellent biocompatibility, and biodegradability. In this review, recent reports on DDSs comprising chitosan/chitosan derivatives supported on carbon nanomaterials, along with their preparation and application, are evaluated. Special emphasis is put on multi-modal approaches to carbon nanomaterials, which made them particularly attractive for biomedical applications. Herein, recent advancement in functionalized carbon nanostructure comprising graphene oxide (GO), carbon nanotubes (CNTs), nanodiamond (ND), fullerene, and carbon quantum dots (CQDs) alongside chitosan/chitosan derivatives as drug vessels are discussed.