OBJECTIVE: To investigate the in vitro transdermal absorption properties of galangin and effects of different penetration enhancers on its transdermal behaviors, and provide reference for developing skin preparations using galangin as APIs in the treatment of vitiligo. METHODS: HPLC was used to determine the galangin content. Using cumulative permeation rate (Q) and the transdermal rate (J) of galangin as indexes, the effect of absorption of receiving solution [20%, 40% polyethylene glycol 400 (PEG400) solution and 30% ethanol solution] and rotating rate (200, 300, 400 r/min) on galangin in complete skin of mice were investigated, as well as the azone (1%, 3%, 5%) and propylene glycol (10%, 20%, 40%) alone or combination on its penetration promotion. And the transdermal properties of galangin in complete skin, exfoliating skin, dermis skin of rats and mice were detected. RESULTS: The best permeability of complete skin of mice showed in 40% PEG400 solution at rotating speed of 300 r/min with 5% azone alone, J was 3.257 0 μg/(cm2·h). Js of complete skin, exfoliating skin, dermis skin of mice were 2.719 9, 34.016, 33.874 μg/(cm2·h), respectively; and those of rats were 0.499 6, 9.512 4, 17.406 μg/(cm2·h). CONCLUSIONS: Galangin can penetrate the complete skin of mice and rats, however, the penetration quantity is far lower than exfoliating skin and dermis skin.