Chitosan-based nanoparticles (chitosan-based nanocomposites; chitosan nanoparticles; ChNPs) are promising materials that are receiving a lot of attention in the last decades. ChNPs have great potential as nanocarriers. They are able to encapsulate drugs as well as active compounds and deliver them to a specific place in the body providing a controlled release. In the article, an overview has been made of the most frequently used preparation methods, and the developed applications in medicine. The presentation of the most important information concerning ChNPs, especially chitosan’s properties in drug delivery systems (DDS), as well as the method of NPs production was quoted. Additionally, the specification and classification of the NPs’ morphological features determined their application together with the methods of attaching drugs to NPs. The latest scientific reports of the DDS using ChNPs administered orally, through the eye, on the skin and transdermally were taken into account.