Department of Pharmaceutical Sciences, School of Pharmacy, University of Connecticut, Storrs, Connecticut 06269, USA.
J Pharm Sci. 2012 Feb;101(2):444-63. doi: 10.1002/jps.22779. Epub 2011 Oct 4.
Aqueous solubility of an active pharmaceutical ingredient is an important consideration to ensure successful drug development. Mesoporous materials have been investigated as an amorphous drug delivery system owing to their nanosized capillaries and large surface areas. The complex interactions of crystalline compounds with mesoporous media and their implication in drug delivery are not well understood. Molecules interacting with porous media behave very differently than those in bulk phase. Their altered dynamics and thermodynamics play an important role in the properties and product performance of the amorphous system. In this review, application of mesoporous silicon dioxide and silicates in drug amorphization is the main focus. First, as background, the nature of gas-porous media interactions is summarized. The synthesis of various types of mesoporous silica, which are used by many investigators in this field, is described. Second, the behavior of molecules confined in mesopores is compared with those in bulk, crystalline phase. The molecular dynamics of compounds due to confinement, analyzed using various techniques, and their consequences in drug delivery are discussed. Finally, the preparation and performance of drug delivery systems using mesoporous silica are examined.
药物活性成分的水溶解度是确保药物开发成功的一个重要考虑因素。介孔材料因其纳米级的毛细孔和较大的表面积而被研究作为无定形药物传递系统。由于结晶化合物与介孔介质之间的复杂相互作用及其在药物传递中的影响,人们对此还了解得不够充分。与在本体相中相比,与多孔介质相互作用的分子表现出非常不同的行为。它们的动力学和热力学的改变在无定形系统的性质和产品性能中起着重要作用。在这篇综述中,主要关注介孔二氧化硅和硅酸盐在药物非晶化中的应用。首先,作为背景,总结了气体-多孔介质相互作用的性质。描述了许多研究人员在这一领域中使用的各种类型的介孔二氧化硅的合成。其次,将受限在介孔中的分子的行为与在本体、晶相中的行为进行比较。讨论了由于受限而导致的化合物的分子动力学,以及使用各种技术对药物传递的影响。最后,检查了使用介孔二氧化硅的药物传递系统的制备和性能。