氧化苦参碱负电荷脂质体的制备及理化性质研究

 目的考察氧化苦参碱负电荷脂质体的处方和制备工艺,并研究其理化性质。方法以包封率为主要指标,对不同制备方法进行考察。采用逆相蒸发法制备,以均匀设计筛选优化最佳处方工艺,制备氧化苦参碱负电荷脂质体,并考察脂质体的形态、粒径、Zeta电位、包封率及体外释放度等理化性质。结果逆相蒸发法制备的脂质体在电镜下呈类圆形,粒径分布均匀,平均为253.6 nm,药物包封率为60.17%,Zeta电位为-40.5,体外释放用双指数方程拟合良好。结论氧化苦参碱负电荷脂质体包封率较高,带负电,粒径分布均匀,符合肝靶向要求。

Studies on Preparation of Anionic Oxymatrine Liposomes and Its Physicochemical Properties

OBJECTIVE To investigate the formulation and preparation technique of anionic oxymatrine liposomes, and determine its physicochemical properties. METHODS Liposme was prepared with different method, using entrapment efficiency as the optimized indexes. The uniform design method was used to optimize the formtdation and preparation technique of oxymatrine liposome. Then the shape, particle size, Zeta potential, entrapment efficiency and drug release in vitro was investigated. RESULTS Oxymatrine liposome prepared by reverse phase evaperation was uniform and round; its mean particle size was 253.6 nm; the entrapment efficiency was 60.17; Zeta potential was - 40.5 and the release kinetics of oxymatrine from hposome was conformed to bioexpinential equation. CONCLUSION The entrapment efficiency of oxymatrine liposome with negative charge is good, its particle size distribution is uniform, and owns liver-targeted properties.