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Resveratrol in Medicinal Chemistry: A Critical Review of its Pharmacokinetics, Drug-Delivery, and Membrane Interactions

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Resveratrol is a polyphenol that among other sources occurs in grapes and for this reason, red wines also contain considerable amounts of this compound. Resveratrol is thought to be responsible for the “French Paradox” which associates red wine consumption to the low incidence of cardiovascular diseases. The interest in resveratrol has increased due to its pharmacological effects that include cardio and neuroprotection and several other benefic actions (e.g. antioxidant, anti-inflammatory, anti-carcinogenic and anti-aging).

Despite the therapeutic effects of resveratrol, its pharmacokinetic properties are not favorable since this compound has poor bioavailability being rapidly and extensively metabolized and excreted. To overcome this problem, drug delivery systems have been developed to protect and stabilize resveratrol and to enhance its bioavailability. Herein is presented an up-to-date revision covering the literature reported for nano and microformulations for resveratrol encapsulation that include liposomes, polymeric nanoparticles, solid lipid nanoparticles, lipospheres, cyclodextrins, polymeric microspheres, yeast cells carriers and calcium or zinc pectinate beads.

Regarding the interaction of resveratrol with cell membranes, only few studies have been published so far. However, it is believed that this interaction can be implied in the biological activities of resveratrol since transmembranar proteins are one of its cellular targets. Indeed, resveratrol presents the capacity to modulate the membrane organization which may consequently affect the protein functionality. Therefore, the intracellular effects of resveratrol and the effects of this compound at the membrane level were also revised since their knowledge is essential for understanding the pharmacological and therapeutic activities of this bioactive compound.
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Keywords: Drug-delivery systems; drug-membrane interactions; pharmacokinetics; resveratrol

Document Type: Research Article

Publication date: 2012-04-01

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  • Current Medicinal Chemistry covers all the latest and outstanding developments in medicinal chemistry and rational drug design. Each issue contains a series of timely in-depth reviews written by leaders in the field covering a range of the current topics in medicinal chemistry. Current Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments.
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