Bolko Katarina, Zvonar Alenka, Gašperlin Mirjana
Acta Chim Slov. 2014;61(1):1-10.
One of the greatest challenges in the pharmaceutical science is the improvement of oral bioavailability of poorly soluble drugs. Lately, one of the most attractive approaches has been formulation of lipid based drug delivery systems. However, the emerging popularity of these systems in the last decade has brought to light the need for efficient methods for their in vitro evaluation that would serve as their in vivo behaviour prediction tool. Because lipids are subject to lipid digestion and multiple absorption pathways in vivo, simple dissolution tests are not predictive enough when testing lipid based delivery systems. To assert these needs, the in vitro lipolysis model has been developed, utilizing pancreatic enzymes, bile and phospholipids in a temperature controlled chamber to simulate in vivo digestion. However, with very variable physiological conditions in gastrointestinal tract, this model has not been yet standardised and experiments vary among different laboratories. This review discusses in vivo events following oral application of lipid based delivery, in vitro lipolysis models to emulate them and their future perspectives.
药物科学中最大的挑战之一是提高难溶性药物的口服生物利用度。最近，最具吸引力的方法之一是制备基于脂质的药物递送系统。然而，在过去十年中这些系统日益普及，这凸显了需要有高效的体外评价方法，作为预测其体内行为的工具。由于脂质在体内会经历脂质消化和多种吸收途径，在测试基于脂质的递送系统时，简单的溶出度试验预测性不足。为满足这些需求，已开发出体外脂解模型，在温度可控的腔室中利用胰酶、胆汁和磷脂来模拟体内消化。然而，由于胃肠道生理条件差异很大，该模型尚未标准化，不同实验室的实验也各不相同。本文综述了口服基于脂质的递送系统后的体内事件、模拟这些事件的体外脂解模型及其未来前景。
