Microneedle technique in promoting transdermal delivery of arbutin / 第二军医大学学报

ABSTRACT

Objective: To study the promoting effects of microneedle arrays on transdermal delivery of arbutin by comparing with the effect of chemical penetration enhancer azone. Methods: The 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 X 4.6 mm, 5μm), at room temperature, mobile phase methanol 1×10-3 mol/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 (J s) and the accumulative deposition amount (Qs) were calculated. Results: The 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.