PREPARATION, CHARACTERIZATION, AND EVALUATION OF ANTI-INFLAMMATORY ACTIVITY OF ETORICOXIB LOADED SOLUPLUS® NANOCOMPOSITES

Abstract

Objective: The objective of this study was to prepare and characterize etoricoxib (ECB) loaded Soluplus® nanocomposites to improve its physicochemical properties. The effect of polymer and surfactant concentration on particle size, in vitro percentage dissolution efficiency and the anti-inflammatory activity of nanocomposites were also investigated.Methods: The nanocomposites were prepared by using a freeze-drying technique. The analytical evidence for the formulation of lyophilized nanocomposites in solid state were generated and confirmed by differential scanning calorimetry (DSC), fourier transformation infrared spectroscopy (FTIR), x-ray powder diffractometry (XPRD) and scanning electron microscopy (SEM). The in vitro drug release profile of nanocomposites was compared with pure ECB powder.Results: The nanocomposites of ECB were contained in a nano range with particle size and zeta potential of 63.5 nm and 46.5 mv, respectively. The solubility and dissolution of the nanocomposites were significantly (p<0.001) improved as compared to ECB alone, evidenced by decreased log P values (1.90±0.002) of the nanocomposites. The characterization studies revealed the formation of amorphous nanocomposites of ECB with existence of physical interactions between drug and polymer. The anti-inflammatory activity of nanocomposites evaluated by carrageenan-induced rat paw edema model demonstrated nonsignificant (p>0.05) increase in anti-inflammatory activity as compared to pure ECB.Conclusion: From the results, it could be concluded that the formation of ECB nanocomposites with Soluplus® could be an effective and alternative approach to modify the physicochemical properties of ECB.