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  • Amphipathic polyethyleneglycols effectively prolong the circulation time of liposomes.

Amphipathic polyethyleneglycols effectively prolong the circulation time of liposomes.

FEBS letters (1990-07-30)
A L Klibanov, K Maruyama, V P Torchilin, L Huang
ABSTRACT

Incorporation of dioleoyl N-(monomethoxy polyethyleneglycol succinyl)phosphatidylethanolamine (PEG-PE) into large unilamellar liposomes composed of egg phosphatidylcholine:cholesterol (1:1) does not significantly increase the content leakage when the liposomes are exposed to 90% human serum at 37 degrees C, yet the liposomes show a significant increase in the blood circulation half-life (t1/2 = 5 h) as compared to those without PEG-PE(t1/2 less than 30 min). The PEG-PE's activity to prolong the circulation time of liposomes is greater than that of the ganglioside GM1, a well-described glycolipid with this activity. Another amphipathic PEG derivative, PEG stearate, also prolongs the liposome circulation time, although its activity is less than that of GM1. Amphipathic PEGs may be useful for the sustained release and the targeted drug delivery by liposomes.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
NanoFabTx NanoFlash PEG Lipid Mix, for CIJ synthesis of PEGylated liposomes
Sigma-Aldrich
NanoFabTX-DOTAP Lipid Mix, for synthesis of cationic (DOTAP) liposomes
Sigma-Aldrich
NanoFabTx- COOH Lipid Mix, for synthesis of carboxyl functionalized liposomes
Sigma-Aldrich
NanoFabTx-DC-Chol Lipid Mix, for synthesis of cationic (DC-cholesterol) liposomes
Sigma-Aldrich
NanoFabTx - PEG Lipid Mix, for synthesis of PEGylated liposomes
Sigma-Aldrich
NanoFabTX- NH2 Lipid Mix, for synthesis of amine functionalized liposomes