摘要
目的研究古糖酯脂质体的制备方法，并建立其包封率的测定方法、方法采用反相蒸发法制备古糖酯脂质体，运用正交实验确定最适的制备条件；采用高效凝胶渗透色谱法（HPGPC）测定古糖酯脂质体的包封率、结果采用反相蒸发法制备古糖酯脂质体的最适条件是：磷脂与胆固醇的摩尔比为4：1，古糖酯药物的加入量为1％，脂水相体积比为3：1，在此条件下制备的脂质体包封率可达39．13％。经负染色法观察古糖酯脂质体的形态为圆形或椭圆形，平均粒径为200nm。采用HPG-PC法可有效地分离古糖酯脂质体与游离药物，方法测定的线性范围为0．2～10．0g·L^-1，平均回收率为95．12％，RSD为1．83％（n=5）。结论反相蒸发法制备的古糖酯脂质体包封率高，粒径小，形态稳定。HPGPC方法简便、快捷，重现性好，适合于古糖酯脂质体包封率的测定。
OBJECTIVE To prepare Polyguluronate Sulfate （PGS） liposomes and determine the encapsulation effieiency of PGSliposomes. METHODS PGS liposomes were prepared by reverse-phase evaporation, and orthugonal test was employed to optimize the conditions of preparation. The encapsulation efficiency of PGS liposomes were determined by high performance gel permeation chroma- tography （HPGPC）. RESULTS The optimum conditions for the preparation of PGS liposomes were as follows ： the molar ratio of lecithin to cholesterol was 4： 1, concentration of PGS was 1% and volume ratio of lipid phase to aqueous phase was 3： 1. The encapsulation efficiency of PGS liposomes was up to 39. 13% at the optimum conditions. The shape of PGS liposomes was observed under elec- tron microscope after negative staining. The liposome vesicles were globular or elliptic and the mean diameter was about 200 nm. PGS liposomes and free PGS were separated effectively by HPGPC method. The linear range was 0.2 - 10.0 g · L^-1 and the average recovery was 95.12% with RSD=1.83% （ n = 5 ）. CONCLUSION Reverse-phase evaporation is suitable to prepare PGS liposomes with high encapsulation efficiency and small vesicles. The HPGPC method was proved to be simple and rapid for the encapsulation efficiency determination of PGS liposomes, and results arc reliable and reproducible.
出处
《中国药学杂志》
CAS
CSCD
北大核心
2007年第19期1476-1479,共4页
Chinese Pharmaceutical Journal
基金
国家"十五"重大专项项目资助(2002AA2Z3145)
关键词
古糖酯
脂质体
反相蒸发法
正交设计
包封率
高效凝胶渗透色谱法
Polyguluronate sulfate
liposome
reverse-phase evaporation
orthogonal design
encapsulation efficiency
high perform-ance gel permeation chromatography （HPGPC）
