固体脂质纳米粒内服吸收机制及影响因素研究进展

Research Progress of Absorption Mechanism and Influence Factors after Oral Administration of Solid Lipid Nanoparticles

关键词:  固体脂质纳米粒  内服；吸收机制；影响因素

Key words:  solid lipid nanoparticles  oral administration  absorption mechanism  influence factor

摘要:

大多数兽药由于渗透性、稳定性和溶解性差以至于无法抵御胃肠道化学和酶等不利环境的降解，不能有效突破胃肠道黏膜屏障，导致生物利用度并不理想。如何保护药物的稳定性并突破消化道黏膜屏障从而提高药物的内服吸收是药物研究者急需寻找解决方案的科学难题。固体脂质纳米粒能提高药物的稳定性并通过不同的转运方式突破胃肠道生理学屏障，从而有效提高药物的内服吸收，表现出显著的疗效，具有良好的发展前景。介绍固体脂质纳米粒的内服吸收机制和胃肠道生理学因素如胃肠道内理化环境、黏液屏障、紧密连接、上皮细胞以及上皮下结缔组织，以及纳米粒的粒径、表面修饰和电荷对其吸收效率的影响，以期为药物研究者提供有效的借鉴。

Abstract:

Because of the poor permeability, stability, and solubility, most of the veterinary drugs in the market are unable to withstand the degradation of gastrointestinal tract’s chemistry and enzymes. Because of the same reason, veterinary drugs could not effectively penetrate the barrier of gastrointestinal mucosa and their bioavailability are not satisfactory. How to protect drugs’ stability and penetrate the barrier of digestive tract mucosa to improve the drug intake is a great scientific challenge that urges drug researchers to find out solutions. It is found that solid lipid nanoparticles can effectively improve the stability of drugs and pass across the physiological barrier of gastrointestinal tract by different means. It can also effectively improve the oral absorption of drugs and show significant effectiveness. Therefore, solid lipid nanoparticles have a good development prospect for coming into clinical application. This paper introduces the absorption mechanism of solid lipid nanoparticles and the influence of gastrointestinal physiological factors (e.g., gastrointestinal environment, mucous barrier, tight junction, gastrointestinal epithelial cells and subepithelial connective tissue), and the physical properties of solid lipid nanoparticles (e.g., including particle size, surface modification and electric charge) on its absorption efficiency, which will provide effective reference for drug researchers.