Nanotechnology offers a number of nanoscale implements for medicine. Among these, nanoparticles are revolutionizing the field of drug and gene delivery. Chitosan is a natural polymer which provides a profitable tool to an innovative delivery system due to its inherent physicochemical and biological characteristics. Chitosan nanoparticles are promising drug and gene delivery carriers because of small size, better stability, low toxicity, inexpensiveness, simplicity, easy fabrication and versatile means of administration. Chitosan can also be easily modified chemically due to the presence of reactive functional hydroxide and amine groups. Folic acid is commonly engaged as a ligand, for targeting cancer cells, as its receptor, that transports folic acid into the cells through endocytosis and is over-expressed on the surface of several human epithelial cancer cells. Integrating folic acid into chitosan-based drug delivery inventions directs the systems with a well-organized targeting ability. The present review outlines several illustrations of this versatile system based on folate decorated chitosan, which have shown potential as auspicious delivery systems published over the past few years. In addition, it is probable to formulate chitosan nanocarriers that exhibit manifold usage beyond targeted delivery, such as nanotheranostics and cancer stem cell therapy.