Chitosan is a partially deacetylated polymer obtained from the alkaline deacetylation of chitin, which is a glucose-based, unbranched polysaccharide that occurs widely in nature as the principal component of exoskeletons of crustaceans and insects, as well as of the cell walls of some bacteria and fungi. Chitosan exhibits a variety of physicochemical and biological properties resulting in numerous applications in fields such as waste water treatment, agriculture, fabric and textiles, cosmetics, nutritional enhancement and food processing. In addition to its lack of toxicity and allergenicity, its biocompatibility, biodegradability and bioactivity make it a very attractive substance for diverse applications as a biomaterial in the pharmaceutical and medical fields. This review takes a closer look at the biomedical applications of chitosan microspheres. Based on recent research and existing products, some new and potential future approaches in this fascinating area are discussed.