Enhancing Aceclofenac Solubility and Dissolution with PVP K30 and β-Cyclodextrin

Abstract

Aceclofenac (AC) is a potent non-steroidal anti-inflammatory drug (NSAID) known for its anti-inflammatory, analgesic, and antipyretic properties. Its effectiveness is comparable to other NSAIDs, with a similar onset of action. As a Biopharmaceutical Classification System (BCS) Class II compound, the oral bioavailability of AC is limited by its dissolution rate in the gastrointestinal tract. Enhancing the dissolution rate of AC is crucial for improving its bioavailability and therapeutic efficacy. This study aimed to prepare and characterize solid dispersions of AC using a mixed excipient system of β-cyclodextrin and polyvinylpyrrolidone K30 (PVP K30) as carriers, and to examine their effect on the drug's dissolution rate. Solid dispersions were created via physical mixture and solvent evaporation methods using different ratios of AC to the excipient system. The formulations were evaluated for parameters such as practical yield, drug content, bulk and tapped density, Hausner’s ratio, Carr’s index, angle of repose, and in vitro drug release. The results showed a significant increase in drug release for the solid dispersions compared to the pure drug, with the solvent evaporation method proving more effective than the physical mixture method. Solid dispersion techniques offer numerous benefits by altering drug release characteristics, leading to faster drug release within the body. The study demonstrated that the solubility of poorly soluble drugs like AC can be significantly improved through solid dispersion methods. The use of water-soluble carriers such as PVP K30 and β-cyclodextrin effectively modified the drug release profiles. Solid dispersions of AC with PVP K30 were prepared in drug-to-carrier ratios of 1:1 to 1:5 using the solvent evaporation method, while inclusion complexes with β-cyclodextrin were prepared by the kneading method in similar ratios. The formulations were screened for yield, texture, color, physical characteristics, and suitability.