N-三甲基壳聚糖对雌二醇凝胶透皮促进作用的体外研究

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

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。

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 dif- ference 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.