Effects of a novel pH-sensitive liposome with cleavable esterase-catalyzed and pH-responsive double smart mPEG lipid derivative on ABC phenomenon

Int J Nanomedicine. 2011:6:2053-61. doi: 10.2147/IJN.S24344. Epub 2011 Sep 20.

Abstract

Background: The ABC phenomenon is described as a syndrome of accelerated clearance of polyethylene glycol (PEG)-modified liposomes from the bloodstream when repeatedly injected, with their increased accumulation in the liver and spleen.

Methods: To clarify this immune response phenomenon, we evaluated a novel modified pH-sensitive liposome with a cleavable double smart PEG-lipid derivative (mPEG-Hz-CHEMS).

Results: The ABC phenomenon in mice was brought about by repeated injection of conventional PEG-PE liposomes and was accompanied by a greatly increased uptake in the liver. However, a slight ABC phenomenon was brought about by repeated injection of mPEG-CHEMS liposomes and was accompanied by only a slightly increased uptake in the liver, and repeated injection of mPEG-Hz-CHEMS liposomes did not induce the ABC phenomenon and there was no increase in liver accumulation. This finding indicates that the cleavable mPEG-Hz-CHEMS derivative could lessen or eliminate the ABC phenomenon induced by repeated injection of PEGylated liposomes.

Conclusion: This research has shed some light on a solution to the ABC phenomenon using a cleavable PEG-Hz-CHEMS derivative encapsulated in nanoparticles.

Keywords: accelerated blood clearance; cleavable; double smart; mPEG-lipid derivates; pH-sensitive liposome.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Female
  • Injections, Intravenous
  • Liposomes* / administration & dosage
  • Liposomes* / chemistry
  • Liposomes* / pharmacokinetics
  • Liver / metabolism
  • Metabolic Clearance Rate / physiology
  • Mice
  • Phosphatidylethanolamines / chemistry*
  • Polyethylene Glycols* / administration & dosage
  • Polyethylene Glycols* / chemistry
  • Polyethylene Glycols* / pharmacokinetics
  • Spleen / metabolism
  • Tissue Distribution

Substances

  • Liposomes
  • Phosphatidylethanolamines
  • 1,2-distearoylphosphatidylethanolamine
  • Polyethylene Glycols
  • monomethoxypolyethylene glycol