N-三甲基壳聚糖对环孢素经皮渗透作用的试验研究

Study on the penetration effect of N-trimethyl chitosan on Cyclosporin

目的考察N-三甲基壳聚糖(N-trim ethyl ch itosan,TMC)作为透皮吸收促进剂的作用大小。方法用壳聚糖及碘甲烷为主要原料,合成季铵化程度为60%的TMC,即TMC60,通过1H-NMR确定其季铵化程度。以2%氮酮为阳性对照,以环孢素为模型药物,以离体小鼠皮肤为屏障,采用预处理法考察2%TMC60对环孢素透过离体皮肤的促进作用。结果经1H-NMR确定合成得到的TMC60季铵化程度为67.2%。体外透皮实验中,累积透过量及稳态透皮速率大小顺序均为:TMC60组>氮酮组>空白组,TMC60的促进作用强度大于同浓度的氮酮(P<0.05)。结论TMC对环孢素具有较好的经皮渗透作用。

OBJECTIVE To study the penetration effect of N-trimethyl chitosan(TMC) on Cyclosporin.METHODS TMC60 was synthesized by a two-step method using chitosan and methyl-iodide.The degree of quaternization(DQ) of TMC was determined by ^(1)H-NMR.The excised mice skin treated by 2% TMC60 or 2% Azone was employed to study the 12h cumulative penetration using Cyclosporin as model drug. RESULTS The DQ of TMC60 was 67.2%.The orders of cumulative penetration(Q) and the steady penetration rate(J) were TMC60 group>Azone group>blank control.The penetration enhancement of TMC60 was stronger than that of Azone(P<0.05).CONCLUSION The results suggested that TMC60 was a promising penetration enhancer for Cyclosporin.