Chitosan, a natural biopolymer derived from chitin, has emerged as a promising nutraceutical with numerous pharmacological applications. Current developments in pharmaceutical research have focused on its ability to improve health and wellness through anti-inflammatory, immunomodulatory, antioxidant, hypolipidemic, hypocholesterolemic, antitumor, and antihypersensitivity properties. These properties make chitosan an ideal constituent for the development of nutraceutical agents with a variety of health benefits. Its biocompatibility, biodegradability, and ability to form multiple complexes enhance its potential as a carrier material in drug delivery and use as an adjuvant in therapies. Furthermore, the increased demand for natural, sustainable, and functional food supplements has increased interest in chitosan-based formulations. This chapter discusses chitosan’s numerous health benefits as a nutraceutical, its underlying mechanisms of action, and its transformative impact on pharmaceutical research and product development. The study of chitosan’s bioactivities opens up new possibilities for nutraceutical innovation, propelling future research into targeted therapies and functional foods.