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采用主动载药法制备抗坏血酸有机锗倍半氧化物脂质体,通过四因素三水平L9(34)正交试验优化制备工艺,评价其质量。采用醋酸钙梯度法考察影响抗坏血酸有机锗倍半氧化物脂质体包封率的不同因素,观察其形态并测定粒径。在4和25℃进行初步稳定性考察。确定最佳处方为60℃孵育3.5 h,磷脂与胆固醇比例12∶1,药物与磷脂质量比1∶20,有机相与水相体积比6∶1。以此最佳处方制得包封率高、性质较稳定的脂质体。脂质体的平均包封率为84.12%,平均粒径为111.6 nm。脂质体于4℃贮存时,渗漏率无显著变化,即4℃为脂质体较理想的储存条件。
Ascorbic acid germanium sesquioxide liposomes were prepared by active drug loading method. The preparation process was optimized by four factors and three levels of L9 (34) orthogonal test to evaluate its quality. Different factors affecting the encapsulation efficiency of ascorbic acid organogermanium sesquioxide liposomes were investigated by calcium acetate gradient method. Morphology was observed and particle size was determined. Preliminary stability studies were performed at 4 and 25 ° C. The optimal prescription was incubated at 60 ℃ for 3.5 h, the ratio of phospholipid to cholesterol was 12: 1, the mass ratio of drug to phospholipid was 1:20, and the volume ratio of organic phase to aqueous phase was 6: 1. The best prescription for the preparation of the encapsulation efficiency, the nature of the more stable liposomes. The average entrapment efficiency of liposomes was 84.12% and the average particle size was 111.6 nm. There was no significant change in the leakage rate when the liposomes were stored at 4 ° C, that is, 4 ° C was the ideal storage condition for the liposomes.