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

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.

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“…Dynamic models represent a novel approach and have significant advantages over static models, including accounting for the effects of peristalsis and transition of proteins between different compartments of the gastrointestinal tract (Dupont & Mackie, ; Picariello, Mamone, Nitride, Addeo, & Ferranti, ). Both static and dynamic models neglect specific issues such as correlation with in vivo models, accounting for different digestion times in individual compartments depending on type of food, predigestion processes in the mouth, and, very significantly, “matrix effects” (McClements et al., ; Rein et al., ). Matrix effects are crucial not only in determining the cleavage sites, but also the kinetics of proteolysis (Barbé et al., ).…”

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