Abstract
Resveratrol, because of its low solubility in water and its high membrane permeability, is collocated in the second class of the biopharmaceutical classification system, with limited bioavailability due to its dissolution rate. Solid dispersion of resveratrol supported on Magnesium DiHydroxide (Resv@MDH) was evaluated to improve solubility and increase bioavailability of resveratrol. Fluorimetric microscopy analysis displays three types of microparticles with similar size: Type 1 that emitted preferably fluorescence at 445 nm with bandwidth of 50 nm, type 2 that emitted preferably fluorescence at 605 nm with bandwidth of 70 nm and type 3 that is non-fluorescent. Micronized pure resveratrol displays only microparticles type 1 whereas type 3 are associated to pure magnesium dihydroxide. Dissolution test in simulated gastric environment resveratrol derived from Resv@MDH in comparison to resveratrol alone displayed better solubility. A 3-fold increase of resveratrol bioavailability was observed after oral administration of 50 mg/kg of resveratrol from Resv@MDH in rabbits. We hypothesize that type 2 microparticles represent magnesium dihydroxide microparticles with a resveratrol shell and that they are responsible for the improved resveratrol solubility and bioavailability of Resv@MDH.
Highlights
Resveratrol is a stilbenic structure polyphenol, initially isolated from the root of the white hellebore
In the present study we investigated that the solid dispersion of resveratrol on magnesium dihydroxide increases its solubility and bioavailability indicating that in some instance this approach could be exploited to enhance biological properties of resveratrol
In this work we report that resveratrol interacts with magnesium dihydroxide at the microparticle level and that this is able to modify its bioavailability
Summary
Resveratrol (trans-3,5,40 -tri-hydroxic-stilbene) is a stilbenic structure polyphenol, initially isolated from the root of the white hellebore Resveratrol became popular in 1992 when it was suggested that it could be the reason behind red wine’s cardio-protective effects (French paradox; [1]), and its popularity increased in 1997 when it was proven that resveratrol was able to prevent colorectal cancer in mice [1]. Resveratrol based compounds present anti-oxidant, anti-inflammatory, anti-viral, cardio-protective, neuro-protective, anti-cancer and anti-angiogenetic activities [1,2,3]. It has been recently observed in obese human subjects that treatment with trans-resveratrol reduces glucose, triglycerides and inflammatory marker levels with a similar effect to the one induced by caloric restriction [4]. The mechanism of action of resveratrol has not been completely defined yet, and for this reason recently studies have been carried out in order to understand the aspects that are still not clear [4]
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