自溶性微针的制备及其对盐酸青藤碱凝胶透皮性能的影响

Preparation of self-dissolving microneedles and its influence on transdermal delivery of sinomenine hydrochloride gel

目的优选出自溶性微针的处方工艺,并考察所制备的微针对盐酸青藤碱凝胶透皮性能的影响。方法采用浇注法制备自溶性微针,穿刺试验考察其机械性能,并采用改良Franz扩散池考察自溶性微针预处理皮肤,对盐酸青藤碱凝胶透皮性能的影响。结果采用浇注法制备自溶性微针,其最佳处方为:基质材料硫酸软骨素和聚乙烯吡咯烷酮(PVP)按照1∶1的比例混合,加入重量比60%的水;所制得的微针针形完整、机械强度良好,能够很好的穿刺铝箔和大鼠皮肤;体外透皮实验显示,自溶性微针使得盐酸青藤碱凝胶的累积渗透量增加了3.62倍。结论优选的自溶性微针的处方与制备工艺简单、可行,可显著提高盐酸青藤碱凝胶的透皮性能,为载药微针的进一步研究提供参考依据。

Objective To optimize the optimal preparation process for self-dissolving microneedles and to explore the percutaneous ab-sorption of sinomenine hydrochloride gel following skin pretreatment with a self-dissolving microneedles patch.Methods Self-dissol-ving microneedles were fabricated by casting.The insertion test of microneedles was to investigate mechanical properties.After pretrea-ting skin with microneedles,we investigated their effect on transdermal delivery of sinomenine hydrochloride gel.Results Self-dissol-ving microneedles were fabricated by casting and the optimized preparation was as follows：50%of chondroitin sulfate and 50%polyvi-nylpyrrolidone （PVP）were mixed,and then 60% of water was added into the matrix.The prepared microneedles were morphologically intact and showed nice mechanical strength after being inserted into aluminum foil and rat skin.In vitro release experiments,the cumu-lative permeation quantity of sinomenine hydrochloride gel was increased by 3.62 times.Conclusion The optimized preparation and the preparation technology of microneedles are simple and reliable.The microneedles enhance the permeability of sinomenine hydrochlo-ride gel.These results provide reference for the further study of drug loaded microneedles.