Enhancing Nutraceutical Performance Using Excipient Foods: Designing Food Structures and Compositions to Increase Bioavailability

TLDR

Oral bioavailability of many bioactives is limited by gastrointestinal events such as restricted release, extensive metabolism, low solubility, poor intestinal permeation, and epithelial efflux. The article proposes that tailoring food matrix composition and structure can enhance bioactive bioavailability by controlling release, transformation, solubilization, transport, absorption, and efflux in the gut. Bioactives can be incorporated into or co‑ingested with excipient foods, notably oil‑in‑water emulsions, to modulate these processes. Using excipient foods offers a new strategy to improve the efficacy of nutraceuticals, supplements, and pharmaceuticals.

Abstract

Abstract The oral bioavailability of many bioactives (pharmaceuticals, dietary supplements, nutrients, and nutraceuticals) is limited because of physicochemical and physiological events that occur within the gastrointestinal tract (GIT) after their ingestion. These events include: (i) restricted liberation from drugs, supplements, or foods; (ii) extensive metabolism or chemical transformation during passage through the GIT; (iii) low solubility in intestinal fluids; (iv) low permeation through the intestinal cell monolayer; and (v) efflux from epithelium cells. Bioactive bioavailability can often be improved by designing the composition and structure of food matrices to control their liberation, transformation, solubilization, transport, absorption, and efflux in the GIT. This article reviews the potential impact of food composition and structure on the oral bioavailability of bioactives, and then shows how this knowledge can be used to design excipient foods that can improve the bioavailability profile of bioactives. The bioactive may be incorporated within an excipient food or co‐ingested with an excipient food. The suitability of oil‐in‐water emulsions as excipient foods is highlighted. The utilization of excipient foods may provide a new strategy for improving the efficacy of nutraceuticals, supplements, and pharmaceuticals.