Passive diffusion of polymeric surfactants across lipid bilayers

J Control Release. 2007 Jul 16;120(1-2):79-87. doi: 10.1016/j.jconrel.2007.03.015. Epub 2007 Mar 31.

Abstract

Self-assembling polymeric surfactant, mmePEG(750)P(CL-co-TMC) [monomethylether poly(ethylene glycol)(750)-poly(caprolactone-co-trimethylene carbonate)], increases drug solubility and crosses an enterocyte monolayer both in vitro and in vivo. The aims of the present work were to investigate whether mmePEG(750)P(CL-co-TMC) polymers can diffuse passively through lipid bilayer using parallel artificial membrane permeability assay (PAMPA) and affect membrane properties using liposomes as model. The mmePEG(750)P(CL-co-TMC) polymer was able to cross by passive diffusion an enterocyte-mimicking membrane in PAMPA at concentration which did not perturb membrane integrity. A weak rigidification associated with a low increase in permeability of liposomal lipid bilayers was observed. These data suggest that polymeric surfactants can cross the lipid membrane by passive diffusion and interact with lipid bilayers.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Cell Membrane Permeability / drug effects
  • Diffusion
  • Dose-Response Relationship, Drug
  • Kinetics
  • Lipid Bilayers / chemistry*
  • Lipid Bilayers / metabolism
  • Liposomes*
  • Mannitol / metabolism
  • Membrane Fluidity / drug effects
  • Membrane Lipids / chemistry*
  • Micelles
  • Models, Chemical
  • Molecular Conformation
  • Particle Size
  • Polyesters / chemistry*
  • Polyesters / pharmacology
  • Polyethylene Glycols / chemistry*
  • Polyethylene Glycols / pharmacology
  • Surface-Active Agents / chemistry*
  • Surface-Active Agents / pharmacology

Substances

  • Lipid Bilayers
  • Liposomes
  • Membrane Lipids
  • Micelles
  • Polyesters
  • Surface-Active Agents
  • monomethyletherpoly(oxyethylene glycol(750))-poly(caprolactone-co-trimethylene carbonate)
  • Mannitol
  • Polyethylene Glycols