Chitosan, a natural based polymer obtained by alkaline deacetylation of chitin, is non-toxic, biocompatible, and biodegradable. These properties make chitosan a good candidate for the development of conventional and novel drug delivery systems. Recently, there has been a growing interest in the chemical modification of chitosan in order to improve its solubility and widen its applications. This new monograph in the ASME-Momentum Press series on Biomedical & Nanomedical Technologies book shows how chemical modification of chitosan is useful for promising materials for the controlled delivery of various types of therapeutic agents.