辣椒碱纳米乳的制备及大鼠透皮实验研究

目的:制备辣椒碱纳米乳并评价其透皮作用。方法:以具有两亲性的苯甲醇作油相,分别以乙醇、1,2-丙二醇和正丁醇作助表面活性剂,以三元相图确定微乳区域,以辣椒碱透皮速率为指标,用单纯形法优化处方。比较优化处方所得辣椒碱纳米乳与其乳膏和水凝胶制剂经大鼠皮肤的稳态透皮速率(Js)。结果:以乙醇和1,2-丙二醇作助表面活性剂的纳米区域面积相当,均大于正丁醇的纳米乳面积。单纯形法可较准确地优化处方,优选处方辣椒碱纳米乳及乳膏和水凝胶的Js分别为17.54、2.78、7.35μg·cm-2·h-1(P<0.01)。结论:所制备的辣椒碱纳米乳具有良好透皮作用。

Preparation and Transdermal Permeation of Capsaicin Nano - emulsion on Rats

OBJECTIVE： To prepare and evaluate the transdermal permeation of capsaicin nano-emulsion. METHODS： The formulation of capsaicin nano - emulsion were optimized by simplex method with steady transdermal permeation rate as the investigation index, with amphiphilie benzyl alcohol as oil phase, and with short chain alcohols, ethanol, propylene glycol and n-butanol as assistant surfactants; and the area of nano- emulsions was determined by ternary phase diagrams. The eapsaiein nano - emulsion prepared with optimized formulation was compared with the eapsaicin ointment and the eapsaiein hydrogel with regard to the steady transdermal rate （Js） in rats. RESULTS： The nano-emulsion with propylene glycol as eosurfactant and that with ethanol as cosurfactant were equivalent in area, and both were larger than that with n - butanol as cosurfactant. Simplex method could accurately optimize the formulations. Js of the optimized capsaiein nano- emulsion, capsaiein ointment, and eapsaiein hydrogel were 17.54, 2.78, and 7.35 μg·cm-2·h-1, respectively（P 〈 0.01） . CONCLUSION ： The nano - emulsion has satisfactory transdermal permeation property.