含胆盐脂质体体外稳定性影响因素的研究  

Influence Factors on in vitro Stability of Liposomes Containing Sodium Glycocholate

作　　者：胡顺文[1,2] 戚建平[2] 卢懿[2] 尹宗宁[1] 吴伟[2] 

机构地区：[1]四川大学华西药学院,四川成都610041 [2]复旦大学药学院,上海201203

出　　处：《中国医药工业杂志》2012年第7期568-571,共4页Chinese Journal of Pharmaceuticals

基　　金：国家重大科学研究计划(2009CB930300);上海市教委曙光计划(10SG05);教育部新世纪优秀人才支持计划(NCET-11-0114)

摘　　要：以钙黄绿素为小分子水溶性荧光探针,采用薄膜分散法制备了平均粒径为150～200 nm的胆盐脂质体(含甘氨胆酸钠,SGC-Lip)和普通脂质体(含胆固醇,CH-Lip)。通过比较两种脂质体在生理范围内的pH、渗透压、胆盐溶液环境中药物的泄漏率,粒径及多分散系数(PDI)的变化来考察胆盐脂质体的稳定性。结果表明,pH和胆盐浓度是影响脂质体稳定性的主要因素,渗透压对脂质体的稳定性影响较小。SGC-Lip在pH 1.2、2.0及低浓度牛黄胆酸钠(<5 mmol/L)溶液中比CH-Lip更稳定。SGC-Lip在不同溶液中粒径和PDI无显著改变,提示胆盐对脂质膜的作用可能是通过对膜的溶蚀形成孔道,而不是使脂质体完全破裂。Liposomes containing sodium glycocholate （SGC-Lip） and conventional liposomes containing cholesterol （CH-Lip） with average diameter of 150 - 200 nm were prepared by the thin-film method with calcein as a small hydrophilic model molecule, respectively. The leakage rate of calcein and the changes of liposomal size and polydispersity index （PDI） within the physiological range of pH, osmotic pressure and bile salt concentration were compared to evaluate the in vitro stability of SGC-Lip. The results showed that pH and bile salt concentration were the main influence factors on the stability of liposomes, while effect of osmotic pressure was not significant. The stability of SGC-Lip was superior to CH-Lip in acidic media （pH 1.2 and 2.0） and at sodium taurocholate concentration of lower than 5 mmol/L. The changes of particle size and PDI of SGC-Lip were not significant in different media, which indicated that the effect of bile salt on lipid member might form channels by corrosion rather than completely rupture liposomes.

关 键 词：脂质体 甘氨胆酸钠 钙黄绿素 稳定性 

分 类 号：R944.9[医药卫生—药剂学]