This chapter highlights the progress in cancer drug delivery by focusing on the novel drug delivery and bioimaging abilities of biomaterials and nanomedicine. Cancer is a globally challenging disease that can emerge in body cells, leading to disruption of the orchestrated cell cycle, evasion of apoptosis, and eventually metastasis. Biomaterials and nanomedicine are highly advanced techniques utilized in various medical areas, including cancer treatment and imaging. Biomaterials and nanomedicine-based technologies have revolutionized the era of cancer treatment by targeting tumor cells, improving internalization efficacy, drug encapsulation, and loading efficacy, as well as being biocompatible and nontoxic to healthy tissue, overcoming the multiresistance and limitations faced by conventional anticancer treatment drugs. This chapter addresses the different perspectives of cancer agent drug therapy, advances in research, and the importance of promising novel technologies for increasing antitumor drug efficacy and survival rate.