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目的:考察寡聚精氨酸壳聚糖(CS-R9)的体内外透皮吸收促进作用。方法:以离体小鼠腹部全皮为皮肤屏障,采用Franz扩散池,以替硝唑(TNZ)溶液为阴性对照,氮酮TNZ溶液为阳性对照,考察CS-R9对TNZ溶液的体外透皮促进作用;以大鼠为实验动物,随机分为阴性组、氮酮组及实验组,分别给予TNZ溶液,氮酮TNZ溶液及CS-R9 TNZ溶液,于给药后不同时间点取血0.5 ml,用HPLC法测定其中TNZ的浓度,考察CS-R9对TNZ在体透皮吸收促进作用。结果:体外试验结果表明与阴性对照相比,CS-R9对TNZ具有显著的透皮吸收促进作用(P<0.05),与同浓度氮酮作用差异无统计学意义(P>0.05);体内透皮实验也表明CS-R9具有显著透皮吸收促进效果,与同浓度氮酮相比,差异无统计学意义(P>0.05),且对药物具有一定的缓释作用。结论:CS-R9对TNZ的透皮吸收具有理想的促进作用,值得进一步研究。
OBJECTIVE: To investigate the in vitro and in vivo transdermal absorption promoting effects of oligoarginine chitosan (CS-R9). Methods: The whole skin of the abdomen of mice was used as the skin barrier. The Franz diffusion cell was used. The TNZ solution was taken as the negative control and the Azone-TNZ solution was used as the positive control. The in vitro transdermal delivery of TNZ solution The rats were randomly divided into negative group, azone group and experimental group. TNZ solution, Azone-TNZ solution and CS-R9 TNZ solution were given respectively. Blood was drawn at different time points after administration of 0.5 ml The concentration of TNZ was determined by HPLC. The effect of CS-R9 on the transdermal absorption of TNZ in vivo was investigated. Results: In vitro experiments showed that CS-R9 had a significant transdermal absorption promoting effect on TNZ compared with the negative control (P <0.05), but no significant difference with the same concentration of Azone (P> 0.05) Skin experiments also showed that CS-R9 had a significant effect of promoting transdermal absorption. Compared with the same concentration of Azone, CS-R9 showed no significant difference (P> 0.05) and had a sustained release effect on the drug. CONCLUSION: CS-R9 has an ideal promoting effect on TNZ transdermal absorption and deserves further study.