Cancer, a malignant disease with a high mortality rate in the world, has not been effectively treated despite the continuous improvement of medical levels. Common drug therapies for cancer treatment have numerous shortcomings including serious side effects, inefficiency, and high cost during the treatment process. As a biopolymer with abundant sources, easy modification, and non-toxicity, chitosan can serve as an ideal carrier for the delivery of anticancer drugs. In this review, we have classified and discussed different forms (nanoscale and non-nanoscale) of anticancer drug carriers where chitosan is used as basic material. The paper has also highlighted their role in cancer treatment and described the release of anticancer drugs from these carriers. Finally, we have proposed the application prospects of chitosan-based delivery systems for anticancer drugs by comparatively evaluating the role of chitosan in anticancer drug delivery.