Chitosan is a natural biopolymer derived from deacetylation of chitin and it has been investigated with interdisciplinary approaches for multitude applications. Chitosan biomaterials possess unique properties such as biocompatibility, biodegradability, non-toxicity, muco-adhesion and a wide range of antibacterial and antifungal activity. Additionally, chitosan is the only cationic polysaccharide in nature and can be chemically modified to derivatives, based on the aim of function and application. The distinctive properties of chitosan and its derivatives have aroused interest in pharmaceutical industries and biomedical fields worldwide. This review discusses the crucial role of chitosan in production of bio-dental materials and accentuates its current profitable utilizations in oral drug delivery system, bone tissue engineering for treatment of periodontitis and dentin-pulp regeneration. Chemical modifications and incorporation of diverse bioactive molecules in order to improve the mechanical and biological characteristics of chitosan have also been discussed.