Amphipathic polyethyleneglycols effectively prolong the circulation time of liposomes

[摘要]

Incorporation of dioleoyl N-(monomethoxy polyethyleneglycol succinyl)phosphotidylethanolamine (PEG-PE) into large unilamellar liposomes composed of egg posphatidylcholine:cholesterol (1:1) does not significantly increase the content leakage when the liposomes are exposed to 90% human serum at 37°C, yet the liposomes show a significant increase in the blood circulation half-life (t = 5 h) as compared to those without PEG-PE(t <30 min). The PEG-PE's activity to prolong the circulation time of liposomes is greater than that of the ganglioside GM₁, awell-described glycolipid with this activity. Another amphipathic PEG derivative, PEG stearate, also prolongs the liposome circulation time, although its activity is less than that ofGM₁. Amphipathic PEGs may be useful for the sustained release and the targeted drug delivery by liposomes.

[学科分类] 生物化学/生物物理

[关键词] Liposome;Polyethyleneglycol;Drug delivery system;PEG;polyethyleneglycol;PEG-OSu;monomethoxy polyethyleneglycol succinimidyl succinate;PE;phosphatidylethanolamine;PEG-PE;dioleoyl N-(monomethoxy polyethyleneglycol succinyl) PE;chol;cholesterol;PC;phosphatidylcholine;DTPA;diethylenetriaminepentaacetic acid;DTPA-SA;DTPA-stearylamide;RES;reticuloendothelial system;PBS;phosphate-buffered saline