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Development of a lozenge for oral transmucosal delivery of trans-resveratrol in humans: proof of concept.

Blanchard OL, Friesenhahn G, Javors MA, Smoliga JM - PLoS ONE (2014)

Bottom Line: 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.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.

View Article: PubMed Central - PubMed

Affiliation: Wilmore Labs, LLC, San Antonio, Texas, United States of America.

ABSTRACT
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.

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Time to peak plasma concentration of tRES following administration of a lozenge in reference to previously reported data.
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pone-0090131-g002: Time to peak plasma concentration of tRES following administration of a lozenge in reference to previously reported data.

Mentions: At baseline, plasma concentration of tRES was below detectable limits and therefore presumed to be zero. Plasma concentrations peaked 15 minutes following lozenge administration (Participant 1: Cmax = 325 ng⋅mL−1; Participant 2: Cmax = 332 ng⋅mL−1). Trans-resveratrol concentrations were below detectable limits at the 30, 45, and 60 post-administration time points. A comparison of these data in reference to previously reported data are presented in FIGURE 1 and FIGURE 2.


Development of a lozenge for oral transmucosal delivery of trans-resveratrol in humans: proof of concept.

Blanchard OL, Friesenhahn G, Javors MA, Smoliga JM - PLoS ONE (2014)

Time to peak plasma concentration of tRES following administration of a lozenge in reference to previously reported data.
© Copyright Policy
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC3935991&req=5

pone-0090131-g002: Time to peak plasma concentration of tRES following administration of a lozenge in reference to previously reported data.
Mentions: At baseline, plasma concentration of tRES was below detectable limits and therefore presumed to be zero. Plasma concentrations peaked 15 minutes following lozenge administration (Participant 1: Cmax = 325 ng⋅mL−1; Participant 2: Cmax = 332 ng⋅mL−1). Trans-resveratrol concentrations were below detectable limits at the 30, 45, and 60 post-administration time points. A comparison of these data in reference to previously reported data are presented in FIGURE 1 and FIGURE 2.

Bottom Line: 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.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.

View Article: PubMed Central - PubMed

Affiliation: Wilmore Labs, LLC, San Antonio, Texas, United States of America.

ABSTRACT
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.

Show MeSH