Amphipathic poly(ethylene glycol) 5000-stabilized dioleoylphosphatidylethanolamine liposomes accumulate in spleen

Biochim Biophys Acta. 1992 Aug 19;1127(3):249-54. doi: 10.1016/0005-2760(92)90228-n.

Abstract

Relatively small liposomes (d less than 200 nm) composed of dioleoylphosphatidylethanolamine (DOPE) and cholesterol (Chol) and containing dioleoyl-N-(monomethoxypoly(ethylene glycol)succinyl)phosphatidylethanolamine (PEG-PE), with PEG of M(r) 5000 (PEG5000-PE), accumulate in the spleen (approximately 40% i.v. injected dose), unlike dioleoylphosphatidylcholine (DOPC)/Chol/PEG5000-PE liposomes of similar size, which show prolonged circulation in the blood. Spleen accumulation was dependent on the injection dose, PEG-PE concentration, and the PEG chain length. The DOPE/Chol/PEG5000-PE liposomes are plasma stable and morphologically indistinguishable from DOPC/Chol/PEG5000-PE liposomes. These results reveal the significance of the matrix lipid in determining the circulation time of PEG-PE-containing liposomes, and are relevant to the design of liposomes which avoid or accumulate in the spleen.

Publication types

  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Animals
  • Cholesterol / metabolism
  • Female
  • Kinetics
  • Liposomes / metabolism*
  • Liposomes / pharmacokinetics
  • Mice
  • Mice, Inbred ICR
  • Phosphatidylethanolamines / metabolism*
  • Phosphatidylethanolamines / pharmacokinetics
  • Polyethylene Glycols / pharmacology*
  • Spleen / metabolism*
  • Structure-Activity Relationship
  • Tissue Distribution

Substances

  • Liposomes
  • Phosphatidylethanolamines
  • Polyethylene Glycols
  • 1,2-dielaidoylphosphatidylethanolamine
  • Cholesterol