Development of solid self-emulsifying drug delivery systems (SEDDS) to improve the solubility of resveratrol

Abstract

The aim of this work was to develop solid self-emulsifying drug delivery systems (SEDDS), using the spray drying technique, for the oral delivery of Resveratrol (RES). The SEDDS were obtained from lipid-based formulations containing cod liver oil as oil phase, and phosphate buffer solution of pH 7.4 as aqueous phase. Three formulations with a different surfactant system composition were tested: soy phosphatidylcholine (SPC)/Eumulgin® HRE 40 (EU)/Sodium Oleate (SO) (system A); FCS/Tween®80 (TW) /SO (system B) and FCS/EU/TW (system C). From pseudoternary phase diagrams, a wide range of combinations was observed to obtain transparent systems. It was possible to incorporate a high concentration of RES in the formulations, observing the greatest incorporation when using system C (21.26 mg/mL). Besides, lactose, maltodextrin, colloidal silicon dioxide (CSD) and CSD: sodium croscarmelose (SC) mixtures were evaluated as adsorbent materials for the spray drying process. Solid SEDDS with the highest percentage of yield were obtained when using CSD (80.12%), CSD:SC 9:1 and 5:5, which may be due to the surface modification to hydrophilic, which reduced the cohesive force among the drug particles. The systems presented appropriate sizes (~1μ) after reconstitution, demonstrating self emulsifing ability. Significant enhancements in RES dissolution were observed from the solid SEDDS, attaining 100% at 45 min with the CSD:SC 5:5 system. From these results, the developed systems are promising to improve the oral bioavailability of RES and other hydrophobic drugs.