Central Nervous System Drug Key Laboratory of Sichuan Province, School of Pharmacy, Southwest Medical University, Luzhou, Sichuan 646000, People's Republic of China.
Int J Nanomedicine. 2020 Aug 24;15:6295-6310. doi: 10.2147/IJN.S257269. eCollection 2020.
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.
口服给药因其安全性高、使用方便、成本低以及患者顺应性好,已成为各种疾病的最常用治疗方案。然而,由于易受到恶劣的胃肠道(GI)环境影响,许多药物在穿过胃肠道黏液和肠上皮时通透性差,口服吸收差,治疗效果有限。近年来,纳米粒给药系统(NDDS)因其独特的优势,如保护药物免受过早降解和与生理环境相互作用、增加细胞内渗透和增强药物吸收,成为研究热点。然而,纳米粒子的理化性质稍有变化,就会显著影响其与生物途径的相互作用,改变药物的口服生物利用度。因此,本综述从两个方面重点讨论了影响口服生物利用度的因素。一方面,这些因素是口服药物递送中的生化和生理屏障。另一方面,这些因素是纳米颗粒的性质,包括纳米颗粒的大小、表面性质和形状。