Development and Characterization Of Solid Dispersion-Based Immediate-Release Meloxicam Pellets Prepared By Extrusion-Spheronization For Enhanced Solubility and Dissolution

Abstract

Meloxicam is a BCS Class II non-steroidal anti-inflammatory drug (NSAID) that has high permeability and lower aqueous solubility, resulting in slow dissolution and delayed onset of action; this is not ideal for the treatment of acute pain. The objective of this study was to develop and characterise immediate-release Meloxicam pellets using the solid dispersion technology along with extrusion-spheronization to improve the release characteristics of the drug in terms of solubility and dissolution to increase its oral bioavailability. Physicochemical properties and BCS classification of the drug were confirmed by preformulation studies. Eight solid dispersions (MSD1–8) were prepared with polyvinylpyrrolidone K30 (PVP K30) in different drug-to-polymer ratios and processed into immediate-release pellets (MF1–8) using the extrusion-spheronization technique, with the inclusion of the functional excipients microcrystalline cellulose, lactose, sodium lauryl sulfate, and croscarmellose sodium. FTIR and DSC analysis confirmed that, compared to pure Meloxicam, the solid dispersions exhibited significantly higher aqueous solubility (3–4 times higher) with statistically significant results (t = 5.39, p = 0.001), which was ascribed to the reduced crystallinity. The resultant pellets were found to have good flow properties, uniform drug content (98.77-101.50 %), narrow particle size distribution and spherical morphology. Dissolution studies demonstrated a very fast release of the drug; more than 90% of Meloxicam was released from MF3 and MF8 formulations in 30 minutes. The results show that co-processing solid dispersion with EX-SPONIZATION is an effective and reproducible approach to tackle the solubility constriction of Meloxicam, in which MF3 is the optimized IR formulation.