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Progress to Improve Oral Bioavailability and Beneficial Effects of Resveratrol

Department of Pharmacy and Health and Nutritional Sciences University of Calabria, Via Pietro Bucci, Arcavacata di Rende, 87036 Cosenza, Italy
Department of Science, University of Basilicata, Viale dell’Ateneo Lucano 10, 85100 Potenza, Italy
Authors to whom correspondence should be addressed.
These authors contributed equally to this work (co-first authors).
Int. J. Mol. Sci. 2019, 20(6), 1381;
Received: 1 February 2019 / Revised: 8 March 2019 / Accepted: 13 March 2019 / Published: 19 March 2019
(This article belongs to the Special Issue Health Benefits of Resveratrol)
Resveratrol (3,5,4′-trihydroxystilbene; RSV) is a natural nonflavonoid polyphenol present in many species of plants, particularly in grapes, blueberries, and peanuts. Several in vitro and in vivo studies have shown that in addition to antioxidant, anti-inflammatory, cardioprotective and neuroprotective actions, it exhibits antitumor properties. In mammalian models, RSV is extensively metabolized and rapidly eliminated and therefore it shows a poor bioavailability, in spite it of its lipophilic nature. During the past decade, in order to improve RSV low aqueous solubility, absorption, membrane transport, and its poor bioavailability, various methodological approaches and different synthetic derivatives have been developed. In this review, we will describe the strategies used to improve pharmacokinetic characteristics and then beneficial effects of RSV. These methodological approaches include RSV nanoencapsulation in lipid nanocarriers or liposomes, nanoemulsions, micelles, insertion into polymeric particles, solid dispersions, and nanocrystals. Moreover, the biological results obtained on several synthetic derivatives containing different substituents, such as methoxylic, hydroxylic groups, or halogens on the RSV aromatic rings, will be described. Results reported in the literature are encouraging but require additional in vivo studies, to support clinical applications. View Full-Text
Keywords: resveratrol; resveratrol bioavailability; resveratrol delivery systems; resveratrol derivatives resveratrol; resveratrol bioavailability; resveratrol delivery systems; resveratrol derivatives
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MDPI and ACS Style

Chimento, A.; De Amicis, F.; Sirianni, R.; Sinicropi, M.S.; Puoci, F.; Casaburi, I.; Saturnino, C.; Pezzi, V. Progress to Improve Oral Bioavailability and Beneficial Effects of Resveratrol. Int. J. Mol. Sci. 2019, 20, 1381.

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