Chitin is one of the most widely present polysaccharidesacross the world.Mainly obtained from crabs and crustaceans, chitosan is obtained on subsequent deacetylation of chitin. Herein, we are reviewing the potential of chitosan as a nanocarrier for delivery of bioactives, for example, anticancer and gene molecules. Utility of chitosan at local sites with reference to its mucoadhesion, plausible chemical modifications, and its processing for selected applications are also discussed. This chapter also endeavors to touch upon the applications of chitosan in colon, nasal, dental and ocular drug delivery, with special emphasis on nanotechnology-based delivery of bioactives.Various studies have also been elaborated on value-added chemical modifications to alter the properties of chitosan, for example, solubility. Nevertheless, the highly recognized characteristics of chitosan (biocompatibility and biodegradability) broaden its realm in wide-ranging biomedical applications of this polysaccharide, particularly using nanotechnology.