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Impact of Various Factors on Pharmacokinetics of Bioactive Polyphenols: An Overview

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Several epidemiological studies throughout the years have suggested that polyphenols from fruits and vegetables promote health and reduce the risk of certain chronic and neurodegenerative diseases. Yet, it has been proved to be extremely difficult to quantitatively establish the benefit afforded by polyphenols, principally due to the limited understanding of the extent of its absorption and metabolic fate. Pharmacokinetics includes the study of the mechanisms of absorption and distribution of an ingested polyphenol, its chemical changes in the body (e.g. by metabolic enzymes), and the effects and routes of excretion of the metabolites. In recent years, there have been major advances in our knowledge of polyphenol absorption and metabolism, and it is apparent that most classes of polyphenols are sufficiently absorbed to have the potential to exert biological effects. The pharmacokinetics of polyphenols includes the same steps as those for orally ingested drugs (LADME) and faces some of the same challenges, including transporters and enzymes. However, unraveling the bioavailability of polyphenols is even more challenging than with drugs, since many other factors, such as the variety in the chemical structure, the food matrix and the gut microbiota, can affect bioavailability of polyphenols during digestion. This review focuses on the most relevant factors that influence polyphenol pharmacokinetics, and also on the most recent technological strategies developed to overcome the poor bioavailability of phenolic compounds and thus increase their potential for greater health benefits.
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Keywords: Bioavailability; food matrix; metabolism; polyphenols; processing

Document Type: Research Article

Publication date: January 1, 2014

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  • Current Drug Metabolism aims to cover all the latest and outstanding developments in drug metabolism and disposition. The journal serves as an international forum for the publication of timely reviews in drug metabolism. Current Drug Metabolism is an essential journal for academic, clinical, government and pharmaceutical scientists who wish to be kept informed and up-to-date with the latest and most important developments. The journal covers the following areas:

    In vitro systems including CYP-450; enzyme induction and inhibition; drug-drug interactions and enzyme kinetics; pharmacokinetics, toxicokinetics, species scaling and extrapolations; P-glycoprotein and transport carriers; target organ toxicity and interindividual variability; drug metabolism and disposition studies; extrahepatic metabolism; phase I and phase II metabolism; recent developments for the identification of drug metabolites and adducts.
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