Amphipathic polyethyleneglycols effectively prolong the circulation time of liposomes

FEBS Letters

Torchilin, Vladimir P.²  Maruyama, Kazuo¹  Huang, Leaf¹  Klibanov, Alexander L.¹ 

[1] Department of Biochemistry, University of Tennessee, 37996 Knoxville, USA;Institute of Experimental Cardiology, 121552 Moscow, USSR

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;   

DOI  :  10.1016/0014-5793(90)81016-H

学科分类：生物化学/生物物理

来源: John Wiley & Sons Ltd.

【 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.

【 授权许可】

Unknown