Improved bioavailability of aceclofenac from spherical agglomerates: development, in vitro and preclinical studies

The objective of present study was to improve the solubility, dissolution rate, micromeritic properties and bioavailability of aceclofenac [NSAID] by formulating its spherical agglomerates. They were prepared with different water soluble polymers [polyvinylpyrrolidone-K30, polyvinylpyrrolidone-K90 and sodium alginate] by using acetone-water-dichloromethane solvent system. The agglomerates were subjected to various physicochemical properties, DSC, IR spectroscopy, scanning electron microscopy [SEM], micromeritic properties and dissolution studies. The in vivo studies [anti-inflammatory, analgesic and pharmacokinetic studies] were conducted in Wistar rats and Swiss albino mice. SEM studies showed that agglomerates were spherical in structure and formed by cluster of small crystals. The agglomerates prepared with polyvinylpyrrolidone-K90 exhibited improved solubility, dissolution rate and micromeritic properties compared to those prepared with other polymers and pure drug. These optimized agglomerates showed rapid analgesic and anti-inflammatory activity besides exhibiting improved bioavailability of drug when compared to pure drug