Solid Dispersion of Resveratrol Supported on Magnesium DiHydroxide (Resv@MDH) Microparticles Improves Oral Bioavailability

白藜芦醇固体分散体负载于二氢氧化镁微粒上(Resv@MDH)可提高口服生物利用度

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作者:Roberto Spogli ,Maria Bastianini ,Francesco Ragonese ,Rossana Giulietta Iannitti ,Lorenzo Monarca ,Federica Bastioli ,Irina Nakashidze ,Gabriele Brecchia ,Laura Menchetti ,Michela Codini ,Cataldo Arcuri ,Loretta Mancinelli ,Bernard Fioretti

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. Keywords: bioavailability; dissolution rate; magnesium dihydroxide; microparticles; resveratrol; solubility.

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