Cancer is one of the major malignant diseases in the world. Current anti tumor agents are restricted during the chemotherapy due to their poor solubility in aqueous media, multidrug resistance problems, cytotoxicity, and serious side effects to healthy tissues. Development of targeted drug nanocarriers would enhance the undesirable effects of anticancer drugs and also selectively deliver them to cancerous tissues. Variety of nanocarriers such as micelles, polymeric nanoparticles, liposomes nanogels, dendrimers, and carbon nanotubes have been used for targeted delivery of anticancer agents. These nanocarriers transfer loaded drugs to desired sites through passive or active efficacy mechanisms. Chitosan and its derivatives, due to their unique properties such as hydrophilicity, biocompatibility, and biodegradability, have attracted attention to be used in nanocarriers. Grafting cancer-specific ligands onto the Chitosan nanoparticles, which leads to ligand-receptor interactions, has been successfully developed as active targeting. Chitosan-conjugated components also respond to external or internal physical and chemical stimulus in targeted tumors that is called environment triggers. In this study, mechanisms of targeted tumor deliveries via nanocarriers were explained; specifically, chitosan-based nanocarriers in tumor-targeting drug delivery were also discussed.