Cancer therapy continues to be a major global concern, with conventional treatments suffering from low efficacy, untargeted drug delivery, and severe side effects. Recent research in nanomedicine suggests that nanoparticles' unique physicochemical properties can be leveraged to surmount the limitations of conventional cancer treatment. Chitosan-based nanoparticles have gained significant attention due to their high drug-carrying capacity, non-toxicity, biocompatibility, and long circulation time. Chitosan is utilized in cancer therapies as a carrier to accurately deliver active ingredients to tumor sites. This review focuses on clinical studies and current market offerings of anticancer drugs. The unique nature of tumor microenvironments presents new opportunities for the development of smart drug delivery systems, and this review explores the design and preparation of chitosan-based smart nanoparticles. Further, we discuss the therapeutic efficacies of these nanoparticles based on various in vitro and in vivo findings. Finally, we present a forward-looking perspective on the challenges and prospects of chitosan-based nanoparticles in cancer therapy, intending to provide fresh ideas for advancing cancer treatment strategies.