Abstract
Resveratrol has emerged as a leading candidate for improving healthspan through potentially slowing the aging process and preventing chronic diseases. The poor bioavailability of resveratrol in humans has been a major concern for translating basic science findings into clinical utility. Although a number of positive findings have emerged from human clinical trials, there remain many conflicting results, which may partially be attributed to the dosing protocols used. A number of theoretical solutions have been developed to improve the bioavailability of resveratrol, including consumption with various foods, micronized powders, combining it with additional phytochemicals, controlled release devices, and nanotechnological formulations. While laboratory models indicate these approaches all have potential to improve bioavailability of resveratrol and optimize its clinical utility, there is surprisingly very little data regarding the bioavailability of resveratrol in humans. If bioavailability is indeed a limitation in the clinical utility of resveratrol, there is a need to further explore methods to optimize bioavailability in humans. This review summarizes the current bioavailability data, focusing on data from humans, and provides suggested directions for future research in this realm.
Highlights
In recent years, resveratrol has gained notoriety as a front runner in the field of anti-aging [1], which is a perilous title when the mechanism of aging itself is poorly defined [2,3,4,5]
The basic parameters associated with drug activity are maximal plasma concentration (Cmax), time to Cmax, half-life (t1/2), and exposure measured by area under curve (AUC)
Skeletal muscle and adipose biopsy is becoming more common in resveratrol human clinical trials [8,111], and it may be incorporated into bioavailability studies
Summary
Resveratrol has gained notoriety as a front runner in the field of anti-aging [1], which is a perilous title when the mechanism of aging itself is poorly defined [2,3,4,5]. Conflicting findings between human and animal have arisen, which have fueled healthy skepticism regarding resveratrol’s ultimate clinical potential Resolutions for such conflicts are made difficult with the observation that the beneficial effects have been attained using dosages far below those required in cell culture [11,21,31]. From the most consistent data presented in the literature, one of the major issues surrounding resveratrol’s future may be achieving adequate bioavailability at tolerable doses—a common issue in translating promising findings from cell culture and animal models into clinical efficacious drugs. The purpose of this review is to briefly describe the approaches that are being explored to improve the bioavailability of resveratrol with a focus on results from human trials exploring resveratrol administration
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