Poly(ethylene glycol)-lipid conjugates inhibit phospholipase C-induced lipid hydrolysis, liposome aggregation and fusion through independent mechanisms

FEBS Lett. 1997 Jul 14;411(2-3):281-6. doi: 10.1016/s0014-5793(97)00716-3.

Abstract

Poly(ethylene glycol)-phosphatidylethanolamine (PEG-PE) conjugates have been introduced in liposomal compositions. The resulting large unilamellar vesicles were subjected to the action of phospholipase C. Enzyme-promoted vesicle aggregation and fusion were assayed in liposomes containing various proportions of PEG-PE. At PEG-PE concentrations above 1 mol% the rate of phospholipid hydrolysis decreases, perhaps because the PEG moiety hinders the enzyme from reaching the membrane surface. At concentrations above 0.1 mol% vesicle aggregation occurs at a slower rate, presumably because of the repulsive barrier properties or surface-grafted PEG. Lipid mixing decreases in parallel with vesicle aggregation. Finally, liposomal fusion rates measured as mixing of vesicle aqueous contents are decreased at or even below 0.1 mol%. The latter inhibition is due, apart from the reduced rates of lipid hydrolysis, vesicle aggregation and lipid mixing, to a PEG-PE-based stabilization of the lipid bilayer structure. Thus the observed low rates of contents mixing arise from three combined and independent inhibitory effects of PEG-PE.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Hydrolysis
  • Kinetics
  • Lipid Bilayers / metabolism
  • Lipid Metabolism
  • Liposomes / chemistry
  • Liposomes / metabolism*
  • Magnetic Resonance Spectroscopy
  • Membrane Fusion / drug effects*
  • Phosphatidylethanolamines / metabolism
  • Phosphatidylethanolamines / pharmacology*
  • Polyethylene Glycols / metabolism
  • Polyethylene Glycols / pharmacology*
  • Temperature
  • Type C Phospholipases / metabolism*

Substances

  • Lipid Bilayers
  • Liposomes
  • Phosphatidylethanolamines
  • dioleoyl-N-(monomethoxypolyethylene glycol succinyl)phosphatidylethanolamine
  • Polyethylene Glycols
  • Type C Phospholipases