Abstract

Resveratrol is a polyphenol present on natural products with a wide range of beneficial properties including antioxidant, anti-inflammatory and chemoprotective effects. However, its low water solubility and rapid presystemic metabolism hampers its absorption and systemic bioavailability. This study investigates the potential of a nanoparticle-based system for the oral delivery of resveratrol in humans and its impact on pharmacokinetics. Resveratrol-loaded zein nanoparticles were prepared and characterized prior to its administration to humans. These nanoparticles displayed a mean size of 331 nm with an encapsulation efficiency of 87%.A single dose of 250 mg of resveratrol was administered to 16 healthy volunteers and the concentrations of resveratrol and its metabolite resveratrol-3-0-D-glucuronide were estimated. The formulation was well tolerated and showed quantifiable plasma levels of resveratrol and its metabolite (Cmax 21.80 and 986.29 ng/mL, respectively). Therefore, this nanoparticle-based formulation has shown a great potential as a nutraceutical for the oral administration of resveratrol.

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