Chitosan is a naturally occurring biodegradable as well as a non-toxic polymer generated from chitin through alkaline deacetylation reaction, and it is insoluble in organic/inorganic solvents and water. Furthermore, chitosan is one of the most plentiful cationic polymers in natural surroundings. Due to its non-toxicity and biocompatibility, chitosan is extensively employed in industrial, biomedical, food, pharmaceutical, environmental, and agricultural industry. Chitosan-based biomaterials exhibit great potential in various biotechnological applications, such as anti-hypertensive therapy, anti-oxidant, anti-microbial, anti-allergic, immunostimulant, cancer therapy, delivery of genetic materials, delivery of bone morphogenetic type-2, wound healing, treatment of wastewater, hypocholesterolemic, and bio-imaging. Therefore, this review mainly focuses on the biotechnological potential of chitosan and its derivatives as well as presents the potential of chitosan-based biomaterial/pharmaceutical for the prevention of various life-threating chronic disorders.