Ursolic, oleanolic and betulinic acids are representative pentacyclic triterpenoids found in various plants and fruits. Despite having marked antitumor potentials, the very poor water solubility of these triterpenes hinders treatment development. Nanotechnology can enhance solubility, stability, bioavailability and phytochemical delivery, improving the therapeutic efficiency of triterpenes. This review focuses on the formulation, characterization and in vitro/in vivo evaluation of several delivery nanosystems used to enhance the physicochemical properties of ursolic, oleanolic and betulinic acids.