淫羊藿苷脂固体质纳米粒制备工艺的优化及其体外释放研究

目的淫羊藿苷固体脂质纳米粒制备方法及处方研究并考察其体外释放情况。方法采用超声分散与高温融溶低温固化结合法制备淫羊藿苷固体脂质纳米粒,考察大豆卵磷脂、胆固醇、投药量、PEG-2000、F-68的用量对包封率、载药量的影响以确定出较优处方配比;用HPLC测定了淫羊藿苷溶液及固体脂质纳米粒在30%甲醇PBS溶液中的体外释放百分率。结果制得的淫羊藿苷固体脂质纳米粒包封率为（98.07±0.15）%,载药量为（6.47±0.14）%;在30%甲醇PBS溶液,淫羊藿苷溶液9 h释放99.97%;淫羊藿苷固体脂质纳米粒72 h累积释放89.75%。结论通过改进后的制备方法优化处方制得固体脂质纳米粒具有较高包封率和载药量,淫羊藿苷固体脂质纳米粒可使淫羊藿苷具有良好的缓释效果。

Study on the optimized preparation and release in vitro of Icarrin-Loaded solid lipid nanoparticles

Objective To optimize the formulation for the preparation of Icariin- loaded solid lipid nanoparticles（ ICA- SLN） and investigate their release in vitro. Methods ICA- SLN was prepared by ultrasonic emulsification technology combined with high temperature melting- cool so lidification method. The optimal preparation was selected and the effects of leithin,cholesterol,PEG- 2000,theoretical drug loading and F- 68 on entrapment efficiency and loading ratio was evaluated. The release rate of ICA and ICA- SLN in PBS solution containing 30% methanol was determined by HPLC. Results The entrapment efficiency and the ratio of loading drug of ICA- SLN were（ 98. 07 ± 0. 15） % and（ 6. 47 ± 0. 14） %,respectively. The cumulative release rate of ICA from PBS solution containing 30% methanol was near 99. 97% in 9 h and over 89. 75% in 72 h. Conclusion The application of the uniform design is useful with high entrapment efficiency and loading ratio through the improved method and ICA- SLN shows well sustained release effects.