Mathot Frédéric, Schanck A, Van Bambeke F, Ariën A, Noppe M, Brewster M, Préat V
Université Catholique de Louvain, Unité de Pharmacie Galénique, UCL, Brussels, Belgium.
J Control Release. 2007 Jul 16;120(1-2):79-87. doi: 10.1016/j.jconrel.2007.03.015. Epub 2007 Mar 31.
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.
自组装聚合物表面活性剂mmePEG(750)P(CL-co-TMC) [单甲醚聚(乙二醇)(750)-聚(己内酯-共-三亚甲基碳酸酯)] 在体外和体内均能提高药物溶解度并穿过肠上皮细胞单层。本研究的目的是使用平行人工膜通透性测定法（PAMPA）研究mmePEG(750)P(CL-co-TMC)聚合物是否能被动扩散穿过脂质双层，并以脂质体为模型研究其对膜性质的影响。mmePEG(750)P(CL-co-TMC)聚合物能够在不干扰膜完整性的浓度下通过被动扩散穿过PAMPA中模拟肠上皮细胞的膜。观察到脂质体脂质双层的通透性有轻微增加并伴有微弱的刚性化。这些数据表明聚合物表面活性剂可通过被动扩散穿过脂质膜并与脂质双层相互作用。
