Abstract：
With the limitation of solubility and dissolution rate of insoluble drugs, following oral administration, they would rifely prove poor and volatile bioavailability, which may fail to realize its therapeutic value. The drug nanocrystals are perceived as effective tactic for oral administration of insoluble drugs attributes to possess many prominent properties such as elevating dissolution rate and saturation solubility, high drug loading capacity, and improving oral bioavailability. Based on these advantages, the application of nanocrystals in oral drug delivery has acquired significant achievement, and so far more than 20 products of drug nanocrystals have been confirmed in the market. However, the oral absorption of drug nanocrystals is still facing huge challenges due to the limitation of many factors. Intrinsic properties of the drugs and complex physiological environment of the intestinal tract are the two most important factors affecting the oral bioavailability of drugs. In addition, the research on the multi-aspect mechanisms of nanocrystals promoting gastrointestinal absorption and bioavailability has been gradually deepened. In this review, we summarized recent advances of the nanocrystals delivered orally, and provided an overview to the research progress for crossing the intestinal tract transport mechanisms of the nanocrystals by some new research techniques. Meanwhile, the factors relevant to the transport of drug nanocrystals were also elaborated in detail. Graphical Abstract.
摘要：
由于难溶性药物的溶解度和溶出度的限制，口服后，他们会证明生物利用度低且易挥发，这可能无法实现其治疗价值。药物纳米晶体被认为是口服不溶性药物的有效策略，具有许多突出的特性，如提高溶出速率和饱和溶解度，高载药量，提高口服生物利用度。基于这些优势,纳米晶体在口服药物递送中的应用取得了显著的成就,到目前为止，已经有超过20种药物纳米晶体产品在市场上得到确认。然而,由于多种因素的限制,药物纳米晶体的口服吸收仍面临着巨大的挑战。药物的内在特性和肠道的复杂生理环境是影响药物口服生物利用度的两个最重要因素。此外,纳米晶体促进胃肠道吸收和生物利用度的多方面机制研究逐渐深入。在这次审查中,我们总结了口服纳米晶体的最新进展，并概述了一些新的研究技术在纳米晶体肠道转运机制方面的研究进展。同时,详细阐述了药物纳米晶体运输的相关因素。图形抽象。
