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目的考察微针对熊果苷皮肤给药的促渗作用,并与化学促渗剂氮酮进行比较。方法采用深反应离子刻蚀技术制备星形硅微针。制备熊果苷水凝胶剂,采用Franz扩散池法,将人体腹部皮肤置于扩散池间,分3组:微针实验组供给室加入熊果苷水凝胶,皮肤采用微针作用;氮酮对照组供给室分别加入含有1%、3%、5%氮酮的熊果苷水凝胶,皮肤无微针作用;空白对照组供给室加入无氮酮熊果苷水凝胶,皮肤无微针作用。分别在1、3、6、12、24、36、48 h等时间点取样,以HPLC法测定接收池、皮肤表皮层和真皮层中的熊果苷含量,液相条件:C18柱(250 mm×4.6 mm,5μm);流动相为甲醇∶1×10-3mol/ml盐酸(5∶95);柱温25℃;流速1 ml/min;检测波长282 nm。求算熊果苷的累积透过量(Qr)、稳态透皮速率(Js)及皮肤累积滞留量(Qs)。结果星形硅微针可以刺穿人体皮肤角质层。HPLC标准曲线方程C=0.000 2A-0.182 9(r=0.999 9),线性范围0.4～50μg/ml、日内精密度和日间精密度分别为2.4%和2.74%,回收率均大于90%。微针作用组的熊果苷累计透过量、稳态透皮速率和表皮累计滞留量均高于5%氮酮组(P<0.01)。结论微针作用皮肤后可显著增加熊果苷皮肤渗透量。
Objective To investigate the effect of micro-acupuncture on the skin penetration of arbutin and compare it with the chemical penetration enhancer Azone. Methods Star-shaped silicon microneedles were prepared by deep reactive ion etching. Preparation of arbutin hydrogel agents, using Franz diffusion cell method, the human abdominal skin placed in the diffusion cell, divided into three groups: micro-needle experimental group donor arbutin hydrogel, the role of the skin with a microneedle; nitrogen Ketone control group feeding room were added 1%, 3%, 5% Azone arbutin hydrogel, the role of the skin without microneedles; blank control group feeding room without azone-free arbutin hydrogel, no skin Microneedle effect. Samples were taken at 1, 3, 6, 12, 24, 36 and 48 h, respectively. The contents of arbutin in the receiving cell, epidermis and dermis were measured by HPLC. × 4.6 mm, 5μm). The mobile phase consisted of methanol: 1 × 10-3mol / ml hydrochloric acid (5:95), the column temperature was 25 ℃, the flow rate was 1 ml / min and the detection wavelength was 282 nm. Calculate arbutin cumulative permeation (Qr), steady-state transdermal rate (Js) and cumulative skin retention (Qs). Results Star silicon microneedles can pierce the cuticle of human skin. The standard curve equation of C was 0.0002A-0.182 9 (r = 0.999 9). The linear range was 0.4 ~ 50μg / ml. The intra-day precision and intraday precision were 2.4% and 2.74%, respectively. The recoveries were both higher than 90%. The cumulative flux of arbutin, the steady-state transdermal rate and the cumulative retention of epidermis in the microneedles group were all higher than those in the 5% Azone group (P <0.01). Conclusion The effect of microneedles on the skin can significantly increase the skin penetration of arbutin.