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目的:制备辣椒碱脂质体及通过体外透皮试验研究其可行性。方法:采用薄膜-超声法制备辣椒碱脂质体,以包封率为指标,在单因素试验基础上采用正交试验法,筛选最优处方。采用改良Franz扩散池进行透皮试验,比较辣椒碱混悬液、辣椒碱脂质体和辣椒碱软膏经大鼠离体皮肤的累积透过量。结果:辣椒碱脂质体的最佳处方:药脂比1∶5,100 mg吐温-80,50mg维生素E,10 ml二氯甲烷,10 ml外水相PBS及pH 6.5,超声8 min。透皮试验12 h累积透过率:辣椒碱脂质体>辣椒碱-PBS混悬液>辣椒碱软膏;辣椒碱脂质体12 h累积透过量最多,且呈现明显的缓释效果。结论:所制备的辣椒碱脂质体包封率高,并具有良好透皮作用和缓释作用,该工艺简便易行。
OBJECTIVE: To prepare capsaicin liposomes and study their feasibility by in vitro transdermal test. Methods: Capsaicin liposomes were prepared by the membrane - ultrasonic method. The optimal encapsulation efficiency was screened by orthogonal test based on single factor test. A modified Franz diffusion cell was used for transdermal test to compare the cumulative permeation of capsaicin suspension, capsaicin liposomes and capsaicin ointment via isolated rat skin. Results: The best prescription of capsaicin liposomes was: the ratio of lipid to lipid was 1: 5, 100 mg of Tween-80, 50 mg of vitamin E, 10 ml of dichloromethane, 10 ml of external aqueous PBS and pH 6.5, sonicated for 8 min. Transdermal test 12 h cumulative transmissibility: capsaicin liposomes> capsaicin-PBS suspension> capsaicin ointment; capsaicin liposomes accumulated the most 12 h, and showed a significant sustained release effect. Conclusion: Capsaicin liposomes prepared with high encapsulation efficiency, and has good transdermal and sustained release effect, the process is simple and easy.