Enhancing intestinal drug solubilisation using lipid-based delivery systems
Enhancing intestinal drug solubilisation using lipid-based delivery systems
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DOI：
10.1016/j.addr.2007.10.014
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发表时间：
2008-03-17
影响因子：
16.1
通讯作者：
Charman, William N.
中科院分区：
文献类型：
--
作者：
Porter, Christopher J. H.;Pouton, Colin W.;Charman, William N.
脂类给药系统在难于溶于水的亲脂性药物的口服给药中得到了越来越多的应用。虽然脂类剂型可以通过几种机制改善口服生物利用度，但促进胃肠溶解仍然是最重要的吸收促进方法，本文首先介绍了使用基于脂质的递送系统来增强药物增溶的机理，并简要回顾了现有的文献，这些文献描述了在给药脂溶液、混悬剂和自乳化制剂后口服生物利用度的增加。随后描述了体外方法的使用，包括分散试验和更复杂的体外脂解模型作为潜在的体内性能的指标，特别关注最近的数据，这些数据表明脂类制剂中存在的表面活性物质的消化可能会影响制剂的性能。最后，基于对我们实验室和其他地方产生的最新数据的分析，提出了一系列用于脂基给药系统配方设计的七项指导原则。(C)2007 Elsevier B.V.保留所有权利。
Lipid-based delivery systems are finding increasing application in the oral delivery of poorly water-soluble, lipophilic drugs. Whilst lipidic dose forms may improve oral bioavailability via several mechanisms, enhancement of gastrointestinal solubilisation remains argueably the most important method of absorption enhancement, This review firstly describes the mechanistic rationale which underpins the use of lipid-based delivery systems to enhance drug solubilisation and briefly reviews the available literature describing increases in oral bioavailability after the administration of lipid Solution, Suspension and self-emulsifying formulations. The use of in vitro methods including dispersion tests and more complex models of in vitro lipolysis as indicators of potential in vivo performance are subsequently described, with particular focus on recent data Which Suggests that the digestion of surfactants present in lipid-based formulations may impact on formulation performance. Finally, a series of seven guiding principles for formulation design of lipid-based delivery systems are suggested based on an analysis of recent data generated in our laboratories and elsewhere. (C) 2007 Elsevier B.V. All rights reserved.