The aim of this review is to provide an overview of the delivery systems of chitosan-based chemotherapy agents that have been developed for the treatment of tumor cancer. Cancer treatment is a challenge that has always provided opportunities in different areas of study, due to its very complexity. Innovative options to make chemotherapy an effective treatment by targeting drugs to cancer cells through different modifications in delivery systems are being investigated. Chitosan, a biopolymer that is obtained from the partial deacetylation of chitin (the second most abundant biopolymer on earth) and is present in the exoskeleton of crustaceans, some insects, and also in the cell wall of some fungi. Chitosan has specific characteristics of solubility, functional groups in its structure, crosslinking power, affinity with other materials, biocompatibility, biodegradability, muco adhesiveness, provides bioavailability of the chemotherapeutic agent on cancer cells, without harming healthy cells. This document compiles some interesting studies on the use of chitosan in conjugation with other agents and safe materials for use in biomedicine, for the design, characterization, and development of new transport systems for chemotherapeutic agents, increasing the efficacy of this therapy in cancer treatment tumors.