Santos Helder A, Peltonen Leena, Limnell Tarja, Hirvonen Jouni
Division of Pharmaceutical Technology, Faculty of Pharmacy, FI-00014 University of Helsinki, Finland.
Curr Pharm Biotechnol. 2013;14(10):926-38. doi: 10.2174/1389201014666131226150404.
Advanced drug delivery formulations are presently recognized as promising tools for overcoming the adverse physicochemical properties of conventional drug molecules, such as poor water solubility, which often leads to poor drug bioavailability. Oral drug delivery is considered as the easiest and most convenient route of drug administration. However, via the current trends utilizing combinatorial chemistry and high throughput screening in drug development, new drug molecules are moving towards lipophilic and poorly water-soluble large molecules, and the oral delivery route is becoming increasingly challenging. In this context, formulation of poorly soluble and/or permeable drugs using mesoporous materials and nanocrystals technology have proven to be highly successful due to the greater surface/volume ratio of these systems, resulting in improvements in dissolution and bioavailability, as well as enhanced drug permeability. This review addresses the issues of poorly water-soluble drugs with a major focus on recent developments in the application of the mesoporous materials (e.g., porous silicon and silica) and nanocrystals in drug delivery applications. In addition, we present several recent examples of the significant potential of these materials for the pharmaceutical field.
先进的药物递送制剂目前被认为是克服传统药物分子不良物理化学性质的有前途的工具,例如水溶性差,这常常导致药物生物利用度低。口服给药被认为是最简便、最方便的给药途径。然而,随着目前药物开发中利用组合化学和高通量筛选的趋势,新的药物分子正朝着亲脂性和水溶性差的大分子发展,口服给药途径正变得越来越具有挑战性。在这种情况下,使用介孔材料和纳米晶体技术来制备难溶性和/或渗透性差的药物已被证明是非常成功的,因为这些体系具有更大的表面/体积比,从而改善了药物的溶出度和生物利用度,并增强了药物渗透性。本综述讨论了水溶性差的药物问题,主要关注介孔材料(如多孔硅和二氧化硅)和纳米晶体在药物递送应用中的最新进展。此外,我们还列举了这些材料在制药领域具有巨大潜力的几个近期实例。