Summary of the research from nutra-ingredients:
Link: http://www.nutraingr...ry-system-Study
In order to test the potential of delivering trans-resveratrol via a lozenge, the researchers tested the solubility of the ingredient in the presence of dextrose, fructose, ribose, sucrose, and xylitol. Results showed that the resveratrol was,“significantly more soluble in the ribose solution than in the other four solutions”, they said, and ribose was subsequently used for the proof of concept test with two healthy human participants.
The volunteers consumed one lozenge containing 146 mg of trans-resveratrol (purchased from Biotivia Longevity Pharmaceuticals) per 2000 mg of lozenge mass.
Data showed that the peak plasma concentrations (Cmax) for resveratrol alone (and not its metabolites) were achieved after only 15 minutes, which is“considerably quicker than the 60–120 minutes reported using traditional free resveratrol tablets,” they said...
“Future research must be conducted to determine if the high plasma levels attained from the optimized resveratrol lozenge hold true across multiple individuals and whether the metabolite profile differs considerably from that obtained from an oral supplement,” they concluded.
Likelihood of seeing a resveratrol lozenge product on the market, soon:
Link: http://www.nutraingr...ry-system-Study
The study was funded by Wilmore Labs, LLC from San Antonio, TX, a start-up company which aims to develop novel formulations for nutraceutical delivery, and the company’s president and CTO, Otis Blanchard, is first author of the paper. The study was performed in collaboration with researchers from the University of Texas Health Science Center at San Antonio, High Point University in North Carolina.
The resveratrol-ribose lozenge is the subject of a pending patent application (2011/0130,469) by Blanchard, who told NutraIngredients-USA that he has been working on the resveratrol lozenge for four years, and the company is actively engaged in pursing commercialization of the product. The bottleneck for further development is investment, he said, and the company is exploring various options to move forward, including crowd-funding.
Full text:
Link: http://www.plosone.o...al.pone.0090131
Development of a Lozenge for Oral Transmucosal Delivery of Trans-Resveratrol in Humans: Proof of Concept
Resveratrol provides multiple physiologic benefits which promote healthspan in various model species and clinical trials support continued exploration of resveratrol treatment in humans. However, there remains concern regarding low bioavailability and wide inter-individual differences in absorption and metabolism in humans, which suggests a great need to develop novel methods for resveratrol delivery. We hypothesized that oral transmucosal delivery, using a lozenge composed of a resveratrol-excipient matrix, would allow resveratrol to be absorbed rapidly into the bloodstream. We pursued proof of concept through two experiments. In the first experiment, the solubility of trans-resveratrol (tRES) in water and 2.0 M solutions of dextrose, fructose, ribose, sucrose, and xylitol was determined using HPLC. Independent t-tests with a Bonferroni correction were used to compare the solubility of tRES in each of the solutions to that in water.tRES was significantly more soluble in the ribose solution (p = 0.0013) than in the other four solutions. Given the enhanced solubility of tRES in a ribose solution, a resveratrol-ribose matrix was developed into a lozenge suitable for human consumption. Lozenges were prepared, each containing 146±5.5 mg tRES per 2000 mg of lozenge mass. Two healthy human participants consumed one of the prepared lozenges following an overnight fast. Venipuncture was performed immediately before and 15, 30, 45, and 60 minutes following lozenge administration. Maximal plasma concentrations (Cmax) for tRES alone (i.e., resveratrol metabolites not included) were 325 and 332 ng⋅mL−1 for the two participants at 15 minute post-administration for both individuals. These results suggest a resveratrol-ribose matrix lozenge can achieve greater Cmax and enter the bloodstream faster than previously reported dosage forms for gastrointestinal absorption. While this study is limited by small sample size and only one method of resveratrol delivery, it does provide proof of concept to support further exploration of novel delivery methods for resveratrol administration.
