草乌甲素可溶性微针的制备、质量评价及体外透皮性能研究

目的 为克服草乌甲素现有给药方式的不足,开展草乌甲素可溶性微针的制备工艺、质量评价及体外透皮性能研究.方法 采用分层浇筑法制备草乌甲素可溶性微针,通过正交法优选最佳处方及制备工艺,并对微针进行质量评价,如微针表观、机械强度、载药量、透皮释放等.结果 草乌甲素可溶性微针的最佳处方及制备工艺为:以35％乙醇溶液作为溶剂,0...

Preparation, quality evaluation and in vitro transdermal properties of Bulleyaconitine A dissolving microneedles

Objective In order to overcome the side effects of the existing administration methods of bulleyaconitine A,the preparation technology,characterization and in vitro transdermal properties of bulleyaconitine A dissolving microneedles were studied.Methods The dissolving microneedles of bulleyaconitine A were prepared by layered pouring method,and the optimal formulation and preparation technology were optimized by orthogonal design.The quality of microneedles was evaluated,such as the appearance,mechanical strength,drug loading,transdermal release,etc.Results The optimal formulation and preparation process of bulleyaconitine A dissolving microneedles were as follows:35%ethanol solution as solvent,0.3 g·mL^-1 hyaluronic acid(HA)and polyvinylpyrrolidone(PVP K30)(4∶6)mixed solution,15%polyvinyl alcohol(PVA)solution as backing substrate,and drying at 35℃to prepare microneedles with drug contents of 150μg,100μg and 70μg,respectively.The results showed that the microneedles had good mechanical strength,and could successfully pierce aluminum foil and pig skin;In vitro transdermal study showed that the drug release of microneedles was 84.67%at 24 h and 96.41%at 48 h.Conclusion The layered dissolving microneedles of bulleyaconitine A were successfully prepared,which can achieve effective transdermal delivery and sustained-release effect.