Diabetes is one of the major health issues that become responsible for several other chronic diseases. A diabetic patient requires the appropriate drug dose that can maintain the glucose level. Different drugs including insulin have been used for diabetes treatment using different routes of administration. The insulin has degradation issues while administering through the oral route and thus require modification to meet the therapeutic needs. New investigations highlighted the potential of chitosan in the form of nanoparticles and microparticles (NPs and MPs) for the development of insulin delivery and controlled release application. The current review provides a brief discussion on the diabetes statistic, current treatments, insulin classifications, insulin delivery using different routes of administration, oral delivery and its barriers, insulin modification, chitosan sources, chitosan preparation techniques, insulin modification with chitosan/chitosan derivatives and chitosan/advanced materials for the development of its controlled release. Further, the kinetics involved in insulin release is discussed. The overview of this research area highlighted the significant development of the insulin delivery system. Insulin is one of the most chosen drugs for diabetic treatment and remained under priority investigation. Among different routes of administration, the oral route is widely investigated for overcoming its enzymatic and chemical barriers. The characteristics of chitosan have highlighted its significant role in drug development. Further, the modified chitosan materials have provided better control of insulin release and its kinetics. However, the literature also indicated some of the limitations and research gaps that need further development. © 2022 Elsevier B.V.