 Nanotherapeutics is rapidly advancing as a solution to the limitations of conventional drug delivery systems in cancer chemotherapy, including lack of selectivity, multi-drug resistance, and poor aqueous solubility, through various mechanisms such as folate and transfer and mediated targeting. Solid lipid nanoparticles, polymeric nanoparticles, mesoporous silica nanoparticles, nanoparticulate chemosensitizer, nanoparticulated paloxamer, magnetic nanoparticles, nanocrystals, albumin-based nanoparticles, liposomal formulation, polymeric micelles, cyclo-dextrin, and chitosin-based nanoparticles. This article was authored by Moody Chidambaram, Arman Vellan, and K. Kuthi-Rezan.