Gigliobianco Maria Rosa, Casadidio Cristina, Censi Roberta, Di Martino Piera
School of Pharmacy, University of Camerino, via S. Agostino, 1, 62032 Camerino, Italy.
Pharmaceutics. 2018 Aug 21;10(3):134. doi: 10.3390/pharmaceutics10030134.
Many approaches have been developed over time to overcome the bioavailability limitations of poorly soluble drugs. With the advances in nanotechnology in recent decades, science and industry have been approaching this issue through the formulation of drugs as nanocrystals, which consist of "pure drugs and a minimum of surface active agents required for stabilization". They are defined as "carrier-free submicron colloidal drug delivery systems with a mean particle size in the nanometer range, typically between 10⁻800 nm". The primary importance of these nanoparticles was the reduction of particle size to nanoscale dimensions, with an increase in the particle surface area in contact with the dissolution medium, and thus in bioavailability. This approach has been proven successful, as demonstrated by the number of such drug products on the market. Nonetheless, despite the definition that indicates nanocrystals as a "carrier-free" system, surface active agents are necessary to prevent colloidal particles aggregation and thus improve stability. In addition, in more recent years, nanocrystal properties and technologies have attracted the interest of researchers as a means to obtain colloidal particles with modified biological properties, and thus their interest is now also addressed to modify the drug delivery and targeting. The present work provides an overview of the achievements in improving the bioavailability of poorly soluble drugs according to their administration route, describes the methods developed to overcome physicochemical and stability-related problems, and in particular reviews different stabilizers and surface agents that are able to modify the drug delivery and targeting.
随着时间的推移，人们已经开发出许多方法来克服难溶性药物的生物利用度限制问题。近几十年来，随着纳米技术的进步，科学界和工业界一直通过将药物制成纳米晶体来解决这个问题，纳米晶体由“纯药物和最少的稳定所需表面活性剂”组成。它们被定义为“平均粒径在纳米范围内，通常在10⁻800nm之间的无载体亚微米胶体药物递送系统”。这些纳米颗粒的主要重要性在于将粒径减小到纳米尺度，增加与溶解介质接触的颗粒表面积，从而提高生物利用度。市场上这类药物产品的数量证明了这种方法的成功。尽管如此，尽管定义中将纳米晶体表明为“无载体”系统，但表面活性剂对于防止胶体颗粒聚集并因此提高稳定性仍是必要的。此外，近年来，纳米晶体的性质和技术作为获得具有改良生物学性质的胶体颗粒的一种手段吸引了研究人员的关注，因此他们现在的兴趣也在于改变药物递送和靶向作用。本工作根据给药途径概述了提高难溶性药物生物利用度方面的成果，描述了为克服物理化学和稳定性相关问题而开发的方法，特别是综述了能够改变药物递送和靶向作用的不同稳定剂和表面活性剂。
