ACECLOFENAC SOLUBILITY ENHANCEMENT BY SONO-PRECIPITATION METHOD: FORMULATION OPTIMIZATION, CHARACTERIZATION AND IN-VITRO EVALUATION

Abstract

Aceclofenac is a commonly used NSAID drug for treatment of pain and inflammation. Aceclofenac has poor water solubility, hence it corresponds to BCS class II drug. Poor solubility leads to poor oral bioavailability, so a challenge for drug delivery. The objective of the present research work is to improve solubility of aceclofenac by using a novel combination of anti-solvent and sono-precipitation technique. Sonoprecipitation has several advantages over conventional methods, like it is cost effective, produces small particle, process is clean, etc. To make this formulation, we dissolved aceclofenac in ethanol and applied 250W sonification for 5 sec followed by 5 sec of interval. This process was repeated for 12 mins and produced micro-sized Aceclofenac dispersion. Further, we characterized and evaluated Aceclofenac dispersion by X-ray powder diffraction (XRPD), Fourier transform infrared (FT-IR) spectroscopy, differential scanning calorimetric (DSC) and in vitro solubility and dissolution rate. The results shows that sonoprecipitation process led to the development of partially amorphous microparticles. The particle size range of 1-3 μm with mean diameter of 1.59 μm. The in-vitro studies indicated that the saturation solubility and dissolution rate of aceclofenac microcrystals were enhanced by 2.5 folds and 2-fold respectively, as compared to crude aceclofenac. In conclusion, the process of combining the antisolvent precipitation under sonication produced small, uniform, and stable aceclofenac microparticles with enhanced dissolution, solubility, and bioavaibility.