Preparation and Optimization of Resveratrol Nanosuspensions by Antisolvent Precipitation Using Box-Behnken Design

Abstract

Resveratrol, a natural polyphenolic component, has inspired considerable interest for its extensive physiological activities. However, the poor solubility of resveratrol circumscribes its therapeutic applications. The purpose of this study was to optimize and prepare resveratrol nanosuspensions using the antisolvent precipitation method. The effects of crucial formulation and process variables (drug concentration, stabilizer, and surfactant contents) on particle size were investigated by utilizing a three-factor three-level Box-Behnken design (BBD) to perform this experiment. Different mathematical polynomial models were used to identify the impact of selected parameters and to evaluate their interrelationship for predictive formulation purposes. The optimal formulation consisted of drug 29.2 (mg/ml), polyvinylpyrrolidone (PVP) K17 0.38%, and F188 3.63%, respectively. The morphology of nanosuspensions was found to be near-spherical shaped by scanning electron microscopy (SEM) observation. The X-ray powder diffraction (XRPD) and differential scanning calorimetry (DSC) analysis confirmed that the nanoparticles were in the amorphous state. Furthermore, in comparison to raw material, resveratrol nanosuspensions showed significantly enhanced saturation solubility and accelerated dissolution rate resulting from the decrease in particle size and the amorphous status of nanoparticles. Meanwhile, resveratrol nanosuspensions exhibited the similar antioxidant potency to that of raw resveratrol. The in vivo pharmacokinetic study revealed that the C max and AUC0→∞ values of nanosuspension were approximately 3.35- and 1.27-fold greater than those of reference preparation, respectively. Taken together, these results suggest that this study provides a beneficial approach to address the poor solubility issue of the resveratrol and affords a rational strategy to widen the application range of this interesting substance.

Testing of resveratrol microemulsion photostability and protective effect against UV induced oxidative stress

“…Similar effects of active substances on droplet size were reported previously when active substances were incorporated into colloidal systems, e.g. microemulsions (14), liposomes (10), nanosuspensions (15). The possibility of RES accumulation in the interfacial layer of nanostructure systems has been discussed earlier (6).…”

Formulation Optimization of Gastro-Retention Tablets of Paeonol and Efficacy in Treatment of Experimental Gastric Ulcer

“…Based on the aforementioned fitting mathematical model, we depicted the corresponding contour map and independent variable on the dependent variable of the three-dimensional (3D) surface figure 37,38) by using Design-Expert (version 8.0.6) software. The results are illustrated in Figs.…”

Resveratrol Nanoparticle’s Formulation - In Diabetic Nephropathy

“…Particularly when particle size is reduced to the nanometric state, the dissolution rate is proportional to the surface area available for dissolution as well-defined by the Noyes-Whitney equation. (Hao, Jifu, et al 2015). …”

“…(Hao, Jifu, et al 2015). 2) Several investigations showed glutaraldehyde as an effective cross-linker that gives stability, shape and an enhanced circulation time to GNPs The aldehyde groups of glutaraldehyde and the amino groups of gelatin undertake Schiff base reaction and form a network assembly, which will support stabilization and controlled release of…”

“…Nano-suspension -raises the probability of obtaining higher therapeutic concentration generating desired pharmacological action (Hao, Jifu, et al 2015).…”