OBJECTIVE: To prepare and characterize Ibuprofen (IBU) nano-powder, and to investigate its transdermal ability in vitro. METHODS: Using chloroform-ethanol (7 ∶ 3, V/V) as organic phase, deionized water as aqueous phase and polysorbate 80 as surfactant, the emulsification method was used to prepare IBU nano-powder. Laser granulometric analysis, Fourier transform infrared spectroscopy (FT-IR), X-ray diffraction (XRD), differential scanning calorimetry (DSC) were used to characterize IBU nano-powder. IBU nano-powder was compared with bulk drug in respects of saturation solubility, dissolution rate and transdermal rate in vitro. RESULTS: The optimum condition was as follows that the concentration of polysorbate 80 was 5 mg/mL; the volume ratio of water phase-organic phase was 40 ∶ 1; the concentration of IBU was 250 mg/mL; homogenate speed was 5 000 r/min; homogenate time was 2 min. Prepared IBU nano-powder was polyporous crumbly coralliform, and its chemical structure kept stable; the nano-powder changed from crystal to amorphous state; the particle size was 179.6 nm, and drug-loading amount was 8.99%; saturation solubility, dissolution rate and transdermal rate of IBU nano-powder were 148, 1.23 and 4.08 times of bulk drug. CONCLUSIONS: The prepared IBU nano-powder shows good water-solubility and percutaneous permeability.