Passive diffusion of polymeric surfactants across lipid bilayers.
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.
Mathot
Frédéric
F
Université Catholique de Louvain, Unité de Pharmacie Galénique, UCL, Brussels, Belgium.
Schanck
A
A
Van Bambeke
F
F
Ariën
A
A
Noppe
M
M
Brewster
M
M
Préat
V
V
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
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