The invention discloses a freeze-dried nanometer powder injection of ursolic acid and a preparing method thereof. It major composes of active material of ursolic acid, complex vehicle of nanometer powder, excipient of freeze-drying. Compared to other popular preparations, its advantages are high target application of liver, concentrate on the affects, increase curative effect, decrease side effect, high dispersity and stability. It is prepared through dissolving ursolic acid as active raw material in medical organic solvent, adding complex vehicle of bean lecithin and stearic acid, stirring while heating until reaction completed, adding distilled water, adding excipient, stirring while heating until reaction completed, filtering with microporous membrane and freeze-drying the filtrate. Its average particle size is 209.5 mm, drug loading is 25.2%. it is for inhibiting and treating liver cancer, decreasing expression of p53, bcl-2 and topo-II.