Drug Delivery, Disposition and Dynamics Monash Institute of Pharmaceutical Sciences, Monash University, Parkville Campus 381 Royal Parade, Parkville, VIC, 3052, Australia.
Pharm Res. 2013 Dec;30(12):3088-100. doi: 10.1007/s11095-013-1108-2. Epub 2013 Aug 7.
The purpose of this study was to investigate the colloidal structures formed on digestion of medium chain triglyceride (MCT) with a specific objective of identifying and characterizing a previously reported vesicular phase, which has been linked to supersaturation and anomalous digestion kinetics, and to evaluate the influence of lipid mass and enzyme inhibition on self assembled structure.
MCT was digested in vitro and nanostructure was monitored in real time using synchrotron small angle X-ray scattering (sSAXS), and morphology was studied using cryogenic transmission electron microscopy (cryo-TEM).
Formation of the putative vesicular phase formed on digestion of MCT was confirmed and its structural attributes were determined. Vesicle formation was dependent on lipid mass and bile salt concentration. The use of enzyme inhibitor for offline analysis of lipolysis samples did influence structural aspects of the digestion medium when compared to real time evaluation.
The formation of a vesicular phase was directly linked to the kinetics of lipid digestion. Vesicle formation is linked to lipid mass, or more specifically the ratio of lipid to bile salts present in the digestion mixture. Inhibition of lipase to halt digestion during sampling for offline analysis must be done with caution as structural aspects were shown to differ for the MCT digests with and without inhibitor present.
本研究旨在探讨中链甘油三酯(MCT)消化过程中形成的胶体结构,具体目的是鉴定和表征先前报道的一种囊泡相,该相与过饱和度和异常消化动力学有关,并评估脂质质量和酶抑制对自组装结构的影响。
MCT 在体外消化,并使用同步加速器小角 X 射线散射(sSAXS)实时监测纳米结构,使用低温透射电子显微镜(cryo-TEM)研究形态。
证实了在 MCT 消化过程中形成的假定囊泡相的形成,并确定了其结构属性。囊泡形成取决于脂质质量和胆汁盐浓度。与实时评估相比,使用酶抑制剂离线分析脂肪酶样品会影响消化介质的结构方面。
囊泡相的形成与脂质消化动力学直接相关。囊泡的形成与脂质质量有关,或者更具体地说,与消化混合物中存在的脂质与胆汁盐的比例有关。为了进行离线分析而在采样时停止脂肪酶消化必须谨慎,因为结果表明,存在和不存在抑制剂的 MCT 消化之间的结构方面存在差异。