Division of Pharmaceutical Chemistry and Technology, Drug Research Program, Faculty of Pharmacy, University of Helsinki, Viikinkaari 5 E, P.O. Box 56, FI-00014 Helsinki, Finland.
Adv Drug Deliv Rev. 2018 Jun;131:101-115. doi: 10.1016/j.addr.2018.06.009. Epub 2018 Jun 18.
The number of poorly soluble drug candidates is increasing, and this is also seen in the research interest towards drug nanoparticles and (nano-)cocrystals; improved solubility is the most important application of these nanosystems. In order to confirm the functionality of these nanoparticles throughout their lifecycle, repeatability of the formulation processes, functional performance of the formed systems in pre-determined way and system stability, a thorough physicochemical understanding with the aid of necessary analytical techniques is needed. Even very minor deviations in for example particle size or size deviation in nanoscale can alter the product bioavailability, and the effect is even more dramatic with the smallest particle size fractions. Also, small particle size sets special requirements for the analytical techniques. In this review most important physicochemical properties of drug nanocrystals and nano-cocrystals are presented, suitable analytical techniques, their pros and cons, are described with the extra input on practical point of view.
难溶性药物候选物的数量正在增加，这在药物纳米粒子和（纳米）共晶体的研究兴趣中也可见一斑；这些纳米系统的最重要应用是提高溶解度。为了确认这些纳米粒子在其整个生命周期中的功能、制剂工艺的可重复性、以预定方式形成的系统的功能性能和系统稳定性，需要借助必要的分析技术来深入了解物理化学性质。即使在例如粒径或纳米级粒径偏差方面出现非常微小的偏差，也会改变产品的生物利用度，而最小粒径分数的影响更为显著。此外，小粒径对分析技术提出了特殊要求。在这篇综述中，介绍了药物纳米晶体和纳米共晶体的最重要物理化学性质，并描述了合适的分析技术，以及它们的优缺点，并从实际角度给出了额外的信息。
