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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。
Using bovine calcein as a small molecule water-soluble fluorescent probe, bile-salt liposomes (including sodium glycocholate SGC-Lip) and ordinary liposomes (average diameter 150-200 nm) Cholesterol, CH-Lip). The stability of bile salt liposomes was investigated by comparing the pH, osmolarity, drug leakage rates, particle size and polydispersity (PDI) of the two liposomes in the physiological range. The results showed that pH and bile salt concentration were the main factors affecting the stability of liposomes, and osmotic pressure had little effect on the stability of liposomes. SGC-Lip is more stable than CH-Lip in pH 1.2, 2.0 and low concentrations of sodium taurocholate (<5 mmol / L). SGC-Lip did not show any significant change in particle size and PDI in different solutions, suggesting that the effect of bile salts on lipid membranes may be due to pore formation by membrane erosion rather than complete rupture of the liposomes.