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脂质体作为药物载体其应用受到限制主要是稳定性不好。脂质体易自身氧化,能被温度升高、金属离子、光照、某些有机分子以及高 pH 所加速,可被金属离子螯合剂及抗氧剂抑制。脂质的氧化可使脂质体膜硬化,显著降低其渗透性。本文研究用α-生育酚及胆固醇阻抑其自动氧化的作用。作者用挤出法制备一定大小的多层脂质体,用聚碳酸酯微孔滤膜(孔径0.8μ)处理,对在 N/2HCl 中的2mg/ml 磷脂酸(Phosphatidic acid,PA)的钠盐用3倍量氯仿-甲醇(10∶1)提取,然后二次用氯仿-甲醇(9∶1)提取,合并提取液完全回收磷脂酸。取磷脂酰胆碱、胆固醇、α-生育酚、硬脂酰胺(氯仿液)及上述磷脂酸液以一定的克分子比置圆底烧瓶,真空干燥。对每克分
Liposomes as a drug carrier limited its application is mainly poor stability. Liposomes are easily oxidized by themselves and can be accelerated by metal ions, light, some organic molecules and high pH, and can be inhibited by metal ion sequestrants and antioxidants. Lipid oxidation can cause the liposomal membrane to harden, significantly reducing its permeability. This article studies the use of alpha-tocopherol and cholesterol to suppress their auto-oxidation. The authors prepared multilamellar liposomes of a certain size by extrusion and treated them with a polycarbonate microporous membrane filter (0.8 [mu] m pore size) for sodium 2 mg / ml Phosphatidic acid (PA) in N / 2HCl The salt was extracted with 3 times the amount of chloroform-methanol (10: 1) and then twice with chloroform-methanol (9: 1). The combined extracts were completely recovered for phosphatidic acid. Take phosphatidylcholine, cholesterol, α-tocopherol, stearic acid amide (chloroform solution) and the above-mentioned phosphatidic acid solution at a certain molar ratio round-bottomed flask, vacuum dried. For every gram of points