Abstract

Ayatallah A. Taelab*, Heba I. Elagamy and Ebtessam A. Essa

ABSTRACT

Trans-resveratrol (RES), among other antioxidants, has recently gained considerable scientific attention due to its protective action against oxidative stress Oromucosal delivery fulfills the urge for more patient compliance, especially the elderly, by formulating convenient dosage forms. Additionally, improved bioavailability is expected due to avoidance of presystemic metabolism of RES. The aim of the present study was to improve the dissolution of RES via modification of its crystalline packing utilizing ethanol- assisted co-grinding with either ascorbic acid (AA) or L-arginine (L-Ar) at 1:1, 1:2, 1:3 molar ratios and prepare fast dissolving buccal films. The composites were evaluated using FTIR, DSC, XRD, and in vitro dissolution. The antioxidant activity of RES after processing was evaluated. Rapid disintegrating buccal films were prepared by casting technique using hydroxypropyl methylcellulose and polyvinylpyrrolidone as film-forming polymers. Physical characterization suggested modulation of RES crystalline nature with possible formation of new species, probably co-crystals. Both excipients improved RES, with L-Ar being superior to AA. The prepared composites preserved the antioxidant activity of RES. The optimized formulations F3 (RES: AA at 1:3) and F5 (RES: L-Ar at 1:2) were successively incorporated in fast disintegrating oral films with prompt RES release of 89.0 and 80.0% after 5 minutes, respectively. The results indicated that treating RES with either AA or L-Ar was a useful tool to improve dissolution. Additionally, rapidly disintegrating buccal film is expected to improve RES bioavailability by avoiding its pre-systemic degradation.