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目的以脱氧胆酸钠(sodium deoxycholate,DOC)为模型胆盐,制备胆盐脂质体,并对其理化性质进行研究。方法采用逆向蒸发法制备胆盐脂质体,以钙黄绿素为模型药,以胆盐脂质体在20mmol·L-1胆盐中的稳定性为指标,考察总脂量、胆固醇与磷脂比、脱氧胆酸钠与脂相的摩尔比等处方因素。采用优化后的处方,考察胆盐脂质体的外观形态,粒径分布及脱氧胆酸钠在胆盐脂质体中的分布情况。结果处方优化后,总脂量、胆固醇与磷脂比及脱氧胆酸钠与脂相的摩尔比应分别为225mg,0.5(w/w)和0.5(mol)。外观形态良好,粒径分布均匀。有效胆盐磷脂摩尔比(Re)为0.26,脱氧胆酸钠在脂相的分配系数(K)为0.21mmol-1。结论处方优化后制备得到的胆盐脂质体的稳定性较好。
OBJECTIVE To prepare bile salt liposomes using sodium deoxycholate (DOC) as model bile salt, and to study its physicochemical properties. Methods The bile salt liposomes were prepared by reverse evaporation method. Calcein was used as a model drug and the stability of bile salt liposomes in 20 mmol·L-1 bile salts was taken as the index. The effects of total lipid, cholesterol and phospholipid ratio, Sodium deoxycholate and lipid molar ratio and other prescription factors. The optimized formulation was used to investigate the appearance and size distribution of bile salt liposomes and the distribution of sodium deoxycholate in bile salts liposomes. Results After optimization, the total lipid, cholesterol and phospholipid ratio and the molar ratio of sodium deoxycholate to lipid phase should be 225mg, 0.5 (w / w) and 0.5 (mol), respectively. Appearance good shape, particle size distribution. The molar ratio of effective bile phospholipid (Re) was 0.26, and the partition coefficient (K) of sodium deoxycholate in the lipid phase was 0.21 mmol-1. Conclusion The stability of the bile salt liposome prepared by the prescription is better.