Oral bioavailability of bioactive compounds; modulating factors, in vitro analysis methods, and enhancing strategies

Abstract

Foods are complex biosystems made up of a wide variety of compounds. Some of them, such as nutrients and bioactive compounds (bioactives), contribute to supporting body functions and bring important health benefits; others, such as food additives, are involved in processing techniques and contribute to improving sensory attributes and ensuring food safety. Also, there are antinutrients in foods that affect food bioefficiency and contaminants that increase the risk of toxicity. The bioefficiency of food is evaluated with bioavailability which represents the amount of nutrients or bioactives from the consumed food reaching the organs and tissues where they exert their biological activity. Oral bioavailability is the result of some physicochemical and biological processes in which food is involved such as liberation, absorption, distribution, metabolism, and elimination (LADME). In this paper, a general presentation of the factors influencing oral bioavailability of nutrients and bioactives as well as the in vitro techniques for evaluating bioaccessibility and is provided. In this context, a critical analysis of the effects of physiological factors related to the characteristics of the gastrointestinal tract (GIT) on oral bioavailability is discussed, such as pH, chemical composition, volumes of gastrointestinal (GI) fluids, transit time, enzymatic activity, mechanical processes, and so on, and the pharmacokinetics factors including BAC and solubility of bioactives, their transport across the cell membrane, their biodistribution and metabolism. The impact of matrix and food processing on the BAC of bioactives is also explained. The researchers’ recent concerns for improving oral bioavailability of nutrients and food bioactives using both traditional techniques, for example, thermal treatments, mechanical processes, soaking, germination and fermentation, as well as food nanotechnologies, such as loading of bioactives in different colloidal delivery systems (CDSs), is also highlighted.