N-三甲基壳聚糖对雌二醇凝胶透皮促进作用的体外研究

目的:研究季铵化程度为60%的N-三甲基壳聚糖对雌二醇凝胶体外透皮吸收的影响。方法:合成季铵化程度为60%的N-三甲基壳聚糖(TMC60),通过1H-NMR确定其季铵化程度。设立含2%TMC60的雌二醇凝胶为TMC60组,含2%氮酮的雌二醇凝胶为阳性组,无促渗剂的雌二醇凝胶为阴性组。通过体外透皮扩散试验得到各组累积透过量(Q),并求出稳态透皮速率(J)。结果:合成得到的TMC60季铵化程度为67.2%。TMC60组的Q和J显著大于阴性组(P<0.05),但与阳性组比较无显著性差异(P>0.05)。结论:2%TMC60与2%氮酮的促渗效果相似,值得进一步研发。

In Vitro Study on the Transdermal Permeation Enhancing Effect of N- trimethyl Chitosan on Estradiol Gels

OBJECTIVE: To study the enhancing effect of N-trimethyl chitosan with degree of quaternization of 60% (TMC60) on the estradiol gel in vitro. METHODS: TMC60 was synthesized and the degree of quaternization was determined by 1H-NMR. Three different kinds of estradiol gels, 2% TMC60 group, 2% azone group and blank control group, were studied respectively. The cumulative penetration Q and steady penetration rate J in vitro were used as the indices. The cumulative penetration was calculated. RESULTS: The degree of quaternization of TMC60 was 67.2%. Significant difference was found the value Q and J of TMC60 group when compared to blank control group(P<0.05), however no significant difference was found when TMC60 group was compared to azone group(P>0.05). CONCLUSION: 2% TMC60 is a penetration enhancer with similar enhancing effect as 2% Azone, which deserves further research.