ObjectiveTo study the promoting effects of microneedle arrays on transdermal delivery of arbutin by comparing with the effect of chemical penetration enhancer azone. MethodsThe microneedles were fabricated with singlecrystal Si as starting material using a series of photolithography, thinfilm deposition, and reactive ion etching techniques. Franzcells were used in the transdermal delivery experiment with human abdominal skin. The study was divided into the following 3 groups: the microneedle group (arbutin hydrogel without penetration enhancer, and the skin was treated with microneedle arrays); the control group (arbutin hydrogels containing 1%, 3%, and 5% azone (W/V), and the skin received no microneedle treatment); and blank control group (arbutin hydrogel without azone, and the skin received no microneedle treatment). Arbutin levels in the receptor solution, epidermis and dermis were determined by HPLC at 1, 3, 6, 12, 24, 36 and 48 h. The analyses were performed with a C18 column (250 mm×4.6 mm, 5 μm), at room temperature, mobile phase methanol1×10-3mol/ml HCl solution (V/V, 595), flow rate 1 ml/min, and detective wavelength 282 nm. The accumulative penetration amount(Qr), steadystate flux(Js) and the accumulative deposition amount(Qs)were calculated. ResultsThe microneedles could pass the human skin. The standard curve was: C=0.000 2A-0.182 9 (r=0.999 9), 0.450 μg/ml. The RSD values of intraday and interday precisions were 2.4% and 2.74%, respectively; and the recovery was higher than 90%.The values of Qr, Js, and Qs in the microneedle group were significantly higher than those in the 5% azone group(P＜0.01). Conclusion Microneedles can greatly promote the skin permeability and deposition of arbutin.