Influence of the steric barrier activity of amphipathic poly(ethyleneglycol) and ganglioside GM1 on the circulation time of liposomes and on the target binding of immunoliposomes in vivo

FEBS Lett. 1991 Jun 24;284(2):263-6. doi: 10.1016/0014-5793(91)80699-4.

Abstract

A series of dioleoyl N-(monomethoxy polyethyleneglycol succinyl)phosphatidylethanolamine (PEG-PE) of different polymer chain length was used in this study. Both the activity of PEG-PE in prolonging the circulation time of liposomes and the relative steric barrier activity of amphipathic polymer, measured by a liposome agglutination assay, were found to be directly proportional to the chain length of PEG-PE (PEG5000-PE greater than PEG2000-PE greater than PEG750-PE). However, PEG5000-PE caused a reduced target binding of immunoliposomes in mice due to its overly strong steric barrier activity. The best PEG-PE species supporting the target binding of immunoliposomes was PEG2000-PE, the activity of which was compatible to that of ganglioside GM1. However, GM1 only showed a weak steric barrier activity, suggesting a different mechanism for this glycolipid.

Publication types

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

MeSH terms

  • Animals
  • Antibodies, Monoclonal
  • Bacterial Proteins / pharmacology
  • Drug Carriers
  • G(M1) Ganglioside / pharmacology*
  • Liposomes / chemistry
  • Liposomes / pharmacokinetics*
  • Lung / metabolism
  • Male
  • Mice
  • Mice, Inbred BALB C
  • Mononuclear Phagocyte System / metabolism
  • Nephelometry and Turbidimetry
  • Phosphatidylethanolamines / pharmacology*
  • Polyethylene Glycols / pharmacology*
  • Streptavidin
  • Structure-Activity Relationship

Substances

  • Antibodies, Monoclonal
  • Bacterial Proteins
  • Drug Carriers
  • Liposomes
  • Phosphatidylethanolamines
  • dioleoyl-N-(monomethoxypolyethylene glycol succinyl)phosphatidylethanolamine
  • G(M1) Ganglioside
  • Polyethylene Glycols
  • Streptavidin