Department of Pharmacy, Faculty of Biological and Health Sciences, Federal University of Jequitinhonha and Mucuri Valleys , Diamantina, Brazil.
Department of Chemistry, Institute of Exact Sciences, Federal University of Minas Gerais , Belo Horizonte, Brazil.
Expert Opin Drug Discov. 2020 Jul;15(7):853-864. doi: 10.1080/17460441.2020.1750591. Epub 2020 Apr 15.
Most drugs used in therapy have low water-solubility, a factor that could reduce their dissolution rate and oral bioavailability, representing a challenge in pharmaceutical development. Nanonization of drugs is the reduction of particles to nanoscale, increasing the surface area and consequently the saturation solubility and dissolution rate and resulting in higher bioavailability.
This review provides an overview of the consequences of the poor water-solubility and the main strategies applied to increase the solubility of poorly water-soluble drugs. The relationship between the biopharmaceutical classification system and the solubilization process of the drug is also considered. Finally, it includes how drug nanoparticles and nanocarriers, especially lipid-based nanosystems, can overcome these challenges and which of these approaches are already available on the market.
Due to the growing importance of nanomedicines, especially for applications in poorly water-soluble drugs, it is important to clearly establish the specifications and quality criteria for nanonized drugs to ensure the quality and safety of nanoparticles.
大多数用于治疗的药物水溶性低,这可能会降低其溶解速率和口服生物利用度,这是药物开发中的一个挑战。药物纳米化是将颗粒减小到纳米级,增加表面积,从而提高饱和溶解度和溶解速率,导致更高的生物利用度。
本篇综述概述了水溶性差的后果,以及用于提高疏水性药物溶解度的主要策略。还考虑了生物制药分类系统与药物溶解过程之间的关系。最后,它包括药物纳米粒子和纳米载体,特别是基于脂质的纳米系统,如何克服这些挑战,以及这些方法中有哪些已经在市场上应用。
由于纳米药物的重要性日益增加,特别是对于疏水性药物的应用,因此明确建立纳米化药物的规格和质量标准非常重要,以确保纳米粒子的质量和安全性。