User:Pushroll/Resveratrol Lozenges
Resveratrol lozenges are intraoral (buccal/sublingual) resveratrol supplements. As a natural compound that has aroused great interest in pharmaceutical, nutritional and cosmetic fields due to the potential beneficial effects it exerts in human health,[1] resveratrol has become a hot ingredient in numerous dietary supplements in the last few years. Among them, most resveratrol supplements are oral pills intended to be swallowed. However, resveratrol lozenges are meant to be kept and consumed in the mouth.
Studies on the absorption, bioavailability, and metabolism of resveratrol in human have shown that the oral bioavailability of resveratrol is extremely low, despite the fact that at least 70% of the resveratrol dose given orally is absorbed. What causes the low bioavailability of resveratrol is that it is rapidly metabolized in intestines and liver due to the first-pass effect. As a result, only a tiny fraction of the resveratrol (<<5%) can reach the bloodstream unchanged.[2][3][4][5]
The veins from the stomach and intestines pass directly through liver, and drugs must first pass through them to enter the bloodstream. Many drugs are extensively metabolized by enzymes in intestines and especially liver. The result is that the therapeutic effects of these drugs are significantly reduced.
Resveratrol lozenge is a way to avoid the problem of first-pass metabolism. The highly vascular intraoral mucosal tissues are the locations for resveratrol absorption. When resveratrol lozenges are being consumed in the oral cavity, the progressively released resveratrol component is absorbed by intraoral mucosal tissues and delivered to the systemic circulation directly. Intraoral delivery allows resveratrol to bypass the first-pass metabolism and thus increase its bioavailability and beneficial effects.
Two studies have shown that intraoral delivery is indeed an effective way to improve resveratrol levels in blood. When 25 mg of resveratrol was swallowed directly, only none to 5 ng/ml of resveratrol could be detected in blood at any time point.[6] In comparison, when merely 1.2 mg of resveratrol in 50 ml solution was retained in the mouth for one minute before swallowing, 37 ng/ml of resveratrol were measured in blood two minutes later.[7] That is an improvement of 154 [(37/5)x(25/1.2)=154] times!! In other words, a resveratrol lozenge containing 10 mg of resveratrol may deliver more intact resveratrol into the bloodstream than a convectional oral resveratrol pill containing 1000 mg of resveratrol.
Therefore, resveratrol lozenges that allow resveratrol to be released to the oral cavity and subsequently delivered across intraoral mucosa is an effective way to increase resveratrol levels in blood circulation. If resveratrol really delivers all the potential benefits,[8] resveratrol lozenges may prove to be an effective resveratrol supplement, or even an effective therapeutic agent in the future.
References[edit]
- ^ S. Pervaiz. “Resveratrol: from Grapevines to Mammalian Biology.” The FASEB Journal. 2003, 17, 1975-1985."[1]"
- ^ T. Walle et al. “High Absorption but Very Low Bioavailability of Oral Resveratrol in Humans.” Drug Metab. Dispos. 2004, 32, 1377-1382."[2]"
- ^ D. J. Boocock et al. “Phase I Dose Escalation Pharmacokinetic Study in Healthy Volunteers of Resveratrol, a Potential Cancer Chemopreventive Agent.” Cancer Epidemiology Biomarkers & Prevention 2007, 16, 1246–1252."[3]"
- ^ A. J. Gescher et al. “Relationship between Mechanisms, Bioavailibility, and Preclinical Chemopreventive Efficacy of Resveratrol: a Conundrum.” Cancer Epidemiol. Biomarkers Prev. 2003, 12, 953-957."[4]"
- ^ M. Singh et al. “Challenges for Research on Polyphenols from Foods in Alzheimer’s Disease: Bioavailability, Metabolism, and Cellular and Molecular Mechanisms.” Journal of Agricultural and Food Chemistry 2008, 56, 4855-4873."[5]"
- ^ T. Walle et al. “High Absorption but Very Low Bioavailability of Oral Resveratrol in Humans.” Drug Metab. Dispos. 2004, 32, 1377-1382."[6]"
- ^ M. Asensi et al. “Inhibition of Cancer Growth by Resveratrol Is Related to Its Low Bioavailability.” Free Radic. Biol. Med. 2002, 33, 387–398."[7]"
- ^ S. Pervaiz. “Resveratrol: from Grapevines to Mammalian Biology.” The FASEB Journal. 2003, 17, 1975-1985."[8]"