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Bioactive compounds that promote beneficial effects on human health, such as phytochemicals, are increasingly being consumed in the form of functional foods or nutraceuticals with the aim of promoting human well-being, health, and performance. However, often nutraceuticals do not show good efficacy in vivo due to their low water solubility, low oral bioavailability, degradation of the gastrointestinal tract, ease of oxidation, and poor absorption by the human body. This problem can often be overcome by nanoencapsulation of bioactive compounds into delivery systems based on biopolymeric nanoparticles. The nanoencapsulation of bioactive compounds can increase their bioavailability due to the size of particles containing these compounds, the availability of these bioactive compounds to the gastrointestinal tract, the ability to penetrate the mucus layer, and by making the compounds available for direct uptake by cells. Biopolymeric nanoparticles can be engineered to survive the gastrointestinal tract and then deliver the bioactive compounds at a certain point, maximizing their potential benefits for human health. In this chapter, bioavailability and delivery mechanisms of nutraceuticals in biopolymer-derived nanoparticles are described and discussed.

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