Chitosan, obtained through deacetylation of chitin, has been shown to a promising biopolymer for the development of nano- and micro-particles. In spite of inherent anti-cancer activity of chitosan, the employment of this carbohydrate polymer for the synthesis of nanoparticles opens a new gate in disease therapy. The properties of chitosan including biocompatibility, biodegradability, and modifiability are vital in enhancing these nanoparticles, allowing for improved solubility and interaction with cellular targets. Among the pathological events, cancer has demonstrated an increase in incidence rate and therefore, the chitosan nanoparticles have been significantly utilized in cancer therapy. The present review emphasizes on the role of stimuli-responsive chitosan nanoparticles in the field of cancer therapy. The stimuli-responsive nanoparticles can release the cargo in the tumor site that not only improves the anti-cancer activity of chemotherapy drugs, but also diminishes their systemic toxicity. The stimuli-responsive chitosan nanoparticles can respond to endogenous and exogenous stimuli including pH, redox and light to release cargo. This improves the specificity towards tumor cells and enhances accumulation of drugs and/or drugs. The light-responsive chitosan nanoparticles can cause photothermal and photodynamic therapy in tumor ablation and provide theranostic feature that is cancer diagnosis and therapy simultaneously.
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