ABSTRACTThe aim of this work is to apply SolutolVRHS15 and TPGS to prepare self-assembled micelles loadingwith ginsenoside Rh2 to increase the solubility of ginsenoside Rh2, hence, improving the antitumorefficacy. Ginsenoside Rh2-mixed micelles (Rh2-M) were prepared by thin film dispersion method. Theoptimal Rh2-M was characterized by particle size, morphology, and drug encapsulation efficiency. Theenhancement of in vivo anti-tumor efficacy of Rh2-M was evaluated by nude mice bearing tumormodel. The solubility of Rh2 in self-assembled micelles was increased approximately 150-folds compared to free Rh2. In vitro results demonstrated that the particle size of Rh2-M is 74.72 ± 2.63 nm(PDI ?0.147 ± 0.15), and the morphology of Rh2-M is spherical or spheroid, and the EE% and LE% are95.27 ± 1.26% and 7.68 ± 1.34%, respectively. The results of in vitro cell uptake and in vivo imagingshowed that Rh2-M could not only increase the cell uptake of drugs, but also transport drug to tumorsites, prolonging the retention time. In vitro cytotoxicity and in vivo antitumor results showed that theanti-tumor effect of Rh2 can be effectively improved by Rh2-M. Therefore, SolutolVRHS15 and TPGScould be used to entrapping Rh2 into micelles, enhancing solubility and antitumor efficacy.