Quercetin is a dietary flavonol that has poor and highly variable bioavailability. Epidemiological studies suggest that higher dietary intakes of quercetin decease cardiovascular disease (CVD) risk. However, experimental findings examining its cardioprotective activities are inconsistent, thereby precluding a full understanding of its health benefits. Bioavailability of dietary constituents is a critical mediator of their health benefits. Thus, a better understanding of the factors regulating quercetin bioavailability is expected to support its potential role in managing CVD risk. This review provides an update on the evidence describing endogenous and exogenous factors responsible for the limited and highly variable bioavailability of quercetin. It focuses on pharmacokinetics studies in clinical and animal models, while also describing strategies aimed at improving quercetin bioavailability to better realize its cardioprotective activities in vivo that are routinely observed in vitro. Although significant advances have been made in understanding determinants of quercetin bioavailability, additional research in controlled trials is needed to more comprehensively examine dose-response effects, whether its cardioprotective activities improve in response to its greater bioavailability, and if the putative health benefits of quercetin are mediated directly or indirectly from one or more of its metabolites generated during xenobiotic metabolism.
Keywords: Bioavailability; Cardioprotective activities; Metabolism; Pharmacokinetics; Quercetin.
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