EFFECT OF MOLECULAR WEIGHT IN AMPHIPATHIC POLYETHYLENEGLYCOL ON PROLONGING THE CIRCULATION TIME OF LARGE UNILAMELLAR LIPOSOMES

概要

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The effect in mice of the molecular weight of polyethyleneglycol on prolonging the circulation time of large unilamellar liposomes (LUVs) was examined using four different distearoyl N-(monomethoxy polyethyleneglycol succinyl) phosphatidylethanolamines (DSPE-PEGs). The molecular weights tested were 1000,2000,5000 and 12000. Incorporation of 6 mol% of DSPE-PEG in LUV composed of distearoylphosphatidylcholine (DSPG) / cholesterol (CH) (1 : 1 in molar ratio) increased the blood circulation half-life significantly more than those without DSPE-PEG derivatives. DSPE-PEGs with molecular weights of 1000 and 2000 prolonged the circulation time of liposomes more than other DSPE-PEGs wiht higher molecular weights, such as 5000 and 12000. Their effects are also higher than ganglioside GM1,a well described glycolipid with this effect. DSPC/CH LUV-incorporated DSPE-PEG with a molecular weight of 2000 displayed a high concentration in the blood, approximately 40% of the dose, 6 h after the injection.
社団法人日本薬学会の論文
1991-06-25