Chitosan (CTS) and graphene (GR) combinations are attracting the interest of drug delivery sectors due to the combined effects of CTS, having exceptional biotic capabilities, and GR, which has excellent physical, chemical, rigid, and spectral properties. CTS and GR composites can be used to create hydrogels, aerogels, scaffolds, films, and nanofibers. The efficiency of CTS/GR composite material in different shapes may be increased even more by including various multifunctional polymeric materials, nano-sized-particles, or proliferation factors due to the ease with which these nanocomposites can be functionalized. Through this context in mind, this chapter describes the most recent discoveries in CTS/GR composites in various forms and compositions in drug delivery applications such as mouth, nostril, eye, oral, lung, sublingual, skin, and anal drug delivery. Future directions for improvement and obstacles for healthcare are also presented.