Karth M G, Higuchi W I, Fox J L
J Pharm Sci. 1985 Jun;74(6):612-7. doi: 10.1002/jps.2600740606.
Studies were designed to demonstrate the use of a silicone rubber membrane diffusion cell in the mechanistic study of cholesterol mass transfer in aqueous media. The method is shown to be simple, precise, and well suited for delineating conditions which facilitate cholesterol transport. Traditional membrane diffusion resistance was determined with cholesterol solubilized in the nonionic surfactant, polyoxyethylene(10)-nonylphenol ether. The use of a charged surfactant additive, either sodium oleate or benzyldimethyltetradecylammonium chloride, reduced cholesterol membrane flux in a manner consistent with a transport barrier residing in the membrane and micelle interfacial regions. Quantitative determination of total transport resistance was good (CV of greater than 95%) for cases more than 99% interface controlled. Interfacial resistance imparted by the charged surfactant additive was essentially abolished by strong electrolyte (sodium chloride). Electrolyte was utilized in either the upstream or the downstream aqueous compartment to enhance cholesterol transport by a mechanism which is consistent with a marked increase in the frequency of micelle collision with the corresponding membrane surface. When the downstream interfacial component of total transport resistance was "short circuited" by electrolyte in sequential transport runs using the same membrane, a "dumping" of cholesterol by the membrane compartment was observed. Limited studies with a second nonionic surfactant, polyoxyethylene(15)-tridecyl ether, suggest that the structure of separate micelle components may also be related to cholesterol mass transfer which occurs via a micelle collision in the interfacial region.
开展多项研究以证明硅橡胶膜扩散池在水介质中胆固醇传质机理研究中的应用。结果表明该方法简单、精确,非常适合描绘促进胆固醇转运的条件。在非离子表面活性剂聚氧乙烯(10)-壬基酚醚中溶解胆固醇来测定传统的膜扩散阻力。使用带电荷的表面活性剂添加剂,即油酸钠或苄基二甲基十四烷基氯化铵,会降低胆固醇的膜通量,其方式与存在于膜和胶束界面区域的传输屏障一致。对于超过99%由界面控制的情况,总传输阻力的定量测定结果良好(变异系数大于95%)。带电荷的表面活性剂添加剂所赋予的界面阻力基本上会被强电解质(氯化钠)消除。在上游或下游水相中使用电解质,通过一种与胶束与相应膜表面碰撞频率显著增加相一致的机制来增强胆固醇的转运。当在使用同一膜的连续转运实验中,总传输阻力的下游界面组分被电解质“短路”时,观察到膜隔室中有胆固醇“倾泻”现象。对第二种非离子表面活性剂聚氧乙烯(15)-十三烷基醚的有限研究表明,单独胶束组分的结构也可能与通过界面区域胶束碰撞发生的胆固醇传质有关。