PREPARATION OF UNILAMELLAR LIPOSOMES OF INTERMEDIATE SIZE (0.1-0.2-MUMM) BY A COMBINATION OF REVERSE PHASE EVAPORATION AND EXTRUSION THROUGH POLYCARBONATE MEMBRANES
PREPARATION OF UNILAMELLAR LIPOSOMES OF INTERMEDIATE SIZE (0.1-0.2-MUMM) BY A COMBINATION OF REVERSE PHASE EVAPORATION AND EXTRUSION THROUGH POLYCARBONATE MEMBRANES
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DOI：
10.1016/0005-2736(80)90558-1
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发表时间：
1980-01-01
期刊：
影响因子：
--
通讯作者：
PAPAHADJOPOULOS, D
中科院分区：
文献类型：
--
作者：
SZOKA, F;OLSON, F;PAPAHADJOPOULOS, D
脂质体可以通过反相蒸发和连续挤出通过聚碳酸酯膜的组合制备。囊泡的直径在0.05-0.5 μ m之间。EM、捕获体积和高碘酸盐氧化反应基团的可用性表明，它们大多是单层的。顺序挤压导致包封效率降低2-4倍，这取决于脂质组成。阴性染色电镜显示，胆固醇与磷脂摩尔比为1:1时，增加了脂质体的平均大小和大小不均一性。在胆固醇与磷脂摩尔比相等的情况下，挤压0.1 μ后的囊泡的平均大小。M膜为0.140 μ M。磷脂酰甘油/磷脂酰胆碱（1:4）组成的囊泡平均大小为0.08 μ m。M挤出后通过0.1 .mu。m膜。中型（0.1-0.2亩）。由该过程形成的囊泡具有3:5的水空间与脂质比，并捕获12%至25%的水相。该方法相对简单、快速，几乎可以定量回收包住大部分水空间的囊泡。
Liposomes can be prepared by a combination of reverse phase evaporation and sequential extrusion through polycarbonate membranes. The vesicles have diameters in the range 0.05-0.5 .mu.m and are mostly unilamellar as indicated by EM, capture volume and availability of reactive groups to periodate oxidation. Sequential extrusion leads to a decrease in the encapsulation efficiency by 2-4-fold, depending upon the lipid composition. The inclusion of cholesterol at a 1:1 molar ratio of cholesterol-to-phospholipid increases the mean size and the size heterogeneity of the liposomes as measured by negative-stain EM. The mean size of vesicles with an equal molar ratio of cholesterol-to-phospholipid after extrusion through a 0.1 .mu.m membrane is 0.140 .mu.m. Vesicles composed of phosphatidylglycerol/phosphatidylcholine (1:4) have a mean size of 0.08 .mu.m after extrusion through a 0.1 .mu.m membrane. The intermediate-size (0.1-0.2 .mu.m) vesicles formed by this process have an aqueous space-to-lipid ratio of 3:5 and capture between 12 and 25% of the aqueous phase. The procedure is relatively simple, rapid and yields almost quantitative recovery of vesicles that encapsulate a large percentage of the total aqueous space.