Thanks to their unique properties, chitosan and chitosan-based materials have numerous applications in the field of biomedicine, especially in drug delivery. This book examines biomedical applications of functional chitosan, exploring the various functions and applications in the development of chitosan-based biomaterials. It also describes the chemical structure of chitosan and discusses the relationship between their structure and functions, providing a theoretical basis for the design of biomaterials. Lastly, it reviews chemically modified and composite materials of chitin and chitosan derivatives for biomedical applications, such as tissue engineering, nanomedicine, drug delivery, and gene delivery.