Van Eerdenbrugh Bernard, Van den Mooter Guy, Augustijns Patrick
Laboratory for Pharmacotechnology and Biopharmacy, K.U. Leuven, Gasthuisberg O&N2, Herestraat 49, Box 921, 3000 Leuven, Belgium.
Int J Pharm. 2008 Nov 19;364(1):64-75. doi: 10.1016/j.ijpharm.2008.07.023. Epub 2008 Jul 31.
During the last 10-15 years, the formulation of drugs as nanocrystals has rapidly evolved into a mature drug delivery strategy, with currently five products on the market. The major characteristic of these systems is the rapid dissolution velocity, enabling bioavailability enhancement after oral administration. This mini-review focuses on recent advances with respect to three topics considering drug nanocrystals. The first topic is nanosuspension stabilization. A current literature status is provided and special attention is given to studies attempting to extend our physicochemical understanding of the underlying principles. The second part describes recent advances on miniaturization of nanosuspension production, to enable formulation screening during preclinical development. Finally, literature available on further nanosuspensions solidification is discussed, focussing on the maintenance of the preservation of the rapid dissolution properties of the nanocrystals after further downstream processing.
在过去10到15年里，药物纳米晶体制剂已迅速发展成为一种成熟的药物递送策略，目前有五种产品上市。这些体系的主要特点是溶解速度快，口服给药后可提高生物利用度。本综述聚焦于药物纳米晶体三个方面的最新进展。第一个方面是纳米混悬液的稳定化。介绍了当前的文献状况，并特别关注那些试图深化我们对相关基本原理物理化学理解的研究。第二部分描述了纳米混悬液生产小型化方面的最新进展，以便在临床前开发阶段进行制剂筛选。最后，讨论了有关纳米混悬液进一步固化的现有文献，重点关注纳米晶体在进一步下游加工后如何保持其快速溶解特性。
