目的研究甘草次酸阳离子脂质体的制备方法并考察其药剂学性质。方法采用正交设计筛选处方,乙醇注入法制备甘草次酸脂质体;用葡聚糖凝胶G-50柱分离脂质体和游离药物,用HPLC法测定包封率;用透射电镜观察脂质体的外观形态,并用粒径分析仪测定脂质体的粒径和zeta电位;进一步考察脂质体的释放规律。结果所得脂质体包封率为(91.61±1.16)%;形态为粒径均匀的球形和类球形,粒径为(141±10)nm,Zeta电位为(35.9±5)mV;脂质体的体外释放符合Higuchi方程;具有较好的稳定性。结论优选得到的甘草次酸脂质体处方和制备工艺合理、稳定,其体外释放具有缓释特点。

Objective To prepare and characterize glycyrrhetinic acid cationic liposomes.Methods Liposomes were prepared by ethanol injection technique.An orthogonal test was utilized to optimize the formulation andpreparation of glycyrrhetinic acid liposomes. The unencapsulated glycyrrhetinic acid and liposomes were separated by Sephadex gel G50,the encapsulation efficiency was detected by HPLC.The morphological examination of glycyrrhetinic acid liposomes was performed using transmission electron microscopy. The particle size and Zeta potential of the liposomes were measured The release rate of glycyrrhetinic acid from liposomes was tested Results The liposomes with spherical or ellipsoidal shape and better stability featured the encapsulation efficiency of (91.61±1.16)%,the mean partical size of(141±10) nm,and Zeta potential of (35.9±5)mV.The in vitro release kinetics were consistent with Higuchi equation.The stability of glycyrrhetinic acid liposomes was better.Conclusion The selected formulation and preparation technic of glycyrrhetinic acid liposomes could be rational,stable,and with a sustained feature in vitro release.

国家自然科学基金资助项目(30772790);高等学校博±学科点专项科研基金(20060572012)