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Bioactive peptides (BAPs) derived from food proteins have been widely investigated in recent years for their bioactive and biocompatible properties. The small intestine is the primary site of the gastrointestinal tract where peptide absorption mainly occurs. To exert their biological effects after oral administration, BAPs have to be absorbed and transported across the intestinal epithelial cells into the blood circulation system. Moreover, BAPs in the blood must reach their target organs in an active form at an effective concentration, that is, bioavailability. To obtain a better insight into the transport, cellular uptake and bioavailability of BAPs, this chapter summarizes and discusses the mechanistic transport mechanisms, bioavailability, modulatory factors and future perspectives of BAPs.

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