Botanical preparations present a widespread and secular history of use. In fact, natural matrices possess a rich pool of phytochemicals, with promising biological effects. Among them, phenolic compounds have revealed to confer very important attributes to improve the well-being and longevity of worldwide population. Numerous in vitro studies have been carried out evaluating the wide spectrum of bioactivities of phenolic compounds, including its health effects, but through in vivo experiments some of these previous results cannot be properly confirmed, and considerable variations are observed. Pharmacokinetic parameters, including the assessment of bioavailability and bioefficacy of phenolic compounds, still continue to be largely investigated and considered a great hot topic among the food science and technology researchers. Thus, based on these crucial aspects, this chapter aims to provide an extensive approach about the question of the bioavailability of phenolic compounds, describing its biosynthetic routes and related mechanisms of action; to focus on the current facts and existing controversies, highlighting the importance of in vivo studies and the impact of phenolic compounds on the quality of life and longevity.
