Chitosan is one of the most popular materials in the field of drug delivery due to its adhesivity and biodegradability. Different types of Chitosan based drug carriers have been conceived for various administration routes, such as oral, nasal, transdermal, parenteral, vaginal, cervical and rectal due to its biocompatibility and biodegradability. Chitosan Nanoparticles (NPs) have long been studied as carriers for systemic and targeted drug delivery. Considerable research efforts have been directed towards developing safe and efficient Chitosan NPs-based particulate drug delivery systems. The results indicated that chemical modification of Chitosan NPs can improve their targeting and bioavailability. The main objectives of this review are to study the Chitosan NPs, their preparation methods, characteristics and modification and finally to evaluate their potential applications in drug delivery systems.