Considerable research efforts have been directed towards developing safe and efficient chitosan-based particulate drug delivery systems. The present review outlines the major new findings on the pharmaceutical applications of chitosan-based micro/nanoparticulate drug delivery systems published over the past decade. Methods of their preparation, drug loading, release characteristics, and applications are covered. Chemically modified chitosan or its derivatives used in drug delivery research are discussed critically to evaluate the usefulness of these systems in delivering the bioactive molecules. From a literature survey, it is realized that research activities on chitosan micro/nanoparticulate systems containing various drugs for different therapeutic applications have increased at the rapid rate. Hence, the present review is timely.