Objective:To prepare tranexamic acid ethosomes(TA@ES),and preliminarily investigate their in vitro permeation.Methods:TA@ES were prepared by an ethanol injection-extrusion method.The formulation was studied by a single-factor method,and then optimized by the Box-Behnken design-response surface method.TA@ES prepared according to the optimal prescription were evaluated for their quality and in vitro permeation.Results:The optimal formulation was as follows:the ratio of phospholipids to tranex-amic acid was 3.20∶1,the dosage of cholesterol was 0.615%,and the dosage of ethanol was 19.366%.The mean particle size of the prepared TA@ES was(194.3±4.1)nm,the Zeta potential was(-32.2±2.6)mV,and the encapsulation efficiency was(17.20%±0.89%).The results of in vitro permeation test showed that the TA@ES not only increased the permeation penetration of the drug(4.98 times),but also increased the deep skin retention(1.74 times),as compared to tranexamic acid aqueous solution.Conclusion:The pre-pared TA@ES can improve the percutaneous penetration and deep skin retention of tranexamic acid,which is expected to be a new vehicle for melasma treatment.
关键词
氨甲环酸/醇质体/Box-Behnken设计-响应面法/体外透皮试验
Key words
Tranexamic acid/Ethosomes/Box-Behnken design-response surface method/In vitro per-meation test
维普
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