Abstract: Oral administration has been the most common therapeutic regimen in various diseases because of its high safety, convenience, lower costs, and high compliance of patients. However, susceptible in hostile gastrointestinal (GI) environment, many drugs show poor permeability across GI tract mucus and intestinal epithelium with poor oral absorption and limited therapeutic efficacy. In recent years, nanoparticulate drug delivery systems (NDDS) have become a hot research spot because of their unique advantages including protecting drug from premature degrading and interacting with the physiological environment, increasing intracellular penetration, and enhancing drug absorption. However, a slight change in physicochemistry of nanoparticles can significantly impact their interaction with biological pathways and alter the oral bioavailability of drugs. Hence, this review focuses on the factors affecting oral bioavailability from two aspects. On the one hand, the factors are the biochemical and physiological barriers in oral drugs delivery. On the other hand, the factors are the nanoparticle properties including size, surface properties, and shape of nanoparticles.

Keywords: oral bioavailability, nanoparticle properties, size, shape, surface properties


中文翻译：

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纳米颗粒性质对药物口服生物利用度的影响。

摘要：口服给药由于其高安全性，方便性，较低的成本和患者的高顺应性，已成为各种疾病中最常见的治疗方案。但是，许多药物在敌对的胃肠（GI）环境中易感，因此显示出对胃肠道粘液和肠上皮的渗透性差，口服吸收差，治疗效果有限。近年来，纳米颗粒药物递送系统（NDDS）由于其独特的优势包括保护药物免于过早降解和与生理环境相互作用，增加细胞内渗透以及增强药物吸收而成为研究的热点。然而，纳米粒子的物理化学的轻微变化会显着影响其与生物途径的相互作用，并改变药物的口服生物利用度。因此，本综述从两个方面着眼于影响口腔生物利用度的因素。一方面，因素是口服药物递送中的生化和生理障碍。另一方面，这些因素是纳米颗粒的性质，包括尺寸，表面性质和纳米颗粒的形状。

关键词：口服生物利用度，纳米颗粒性质，大小，形状，表面性质