title: Passive diffusion of polymeric surfactants across lipid bilayers.
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.
authors.affiliation: Université Catholique de Louvain, Unité de Pharmacie Galénique, UCL, Brussels, Belgium.
authors.forename: Frédéric
authors.initials: F
authors.lastname: Mathot
authors.forename: A
authors.initials: A
authors.lastname: Schanck
authors.forename: F
authors.initials: F
authors.lastname: Van Bambeke
authors.forename: A
authors.initials: A
authors.lastname: Ariën
authors.forename: M
authors.initials: M
authors.lastname: Noppe
authors.forename: M
authors.initials: M
authors.lastname: Brewster
authors.forename: V
authors.initials: V
authors.lastname: Préat
mesh_terms: D002463:Cell Membrane Permeability / Q000187:drug effects; D004058:Diffusion; D004305:Dose-Response Relationship, Drug; D007700:Kinetics; D008051:Lipid Bilayers / Q000737:chemistry* / Q000378:metabolism; D008081:Liposomes; D008353:Mannitol / Q000378:metabolism; D008560:Membrane Fluidity / Q000187:drug effects; D008563:Membrane Lipids / Q000737:chemistry*; D008823:Micelles; D008956:Models, Chemical; D008968:Molecular Conformation; D010316:Particle Size; D011091:Polyesters / Q000737:chemistry* / Q000494:pharmacology; D011092:Polyethylene Glycols / Q000737:chemistry* / Q000494:pharmacology; D013501:Surface-Active Agents / Q000737:chemistry* / Q000494:pharmacology
chemical_list: D008051:Lipid Bilayers; D008081:Liposomes; D008563:Membrane Lipids; D008823:Micelles; D011091:Polyesters; D013501:Surface-Active Agents; C513506:monomethyletherpoly(oxyethylene glycol(750))-poly(caprolactone-co-trimethylene carbonate); D008353:Mannitol; D011092:Polyethylene Glycols