Response Surface Methodology-Based In Vitro And In Vivo Evaluation Of Nsaid-Loaded Eudragit Microspheres

Abstract

This study targets on the development and characterization of extended-release microspheres loaded with the nonsteroidal anti-inflammatory drug (NSAID) Aceclofenac, using the Eudragit RS-100 polymer. To use a single emulsion [oil-in-oil] solvents evaporation technique, the microspheres were created, with the impact of three independent variables (poly vinyl acetate, polymer, and stirring speed) evaluated using Design-Expert® Software and response surface methodology. The dependent variables chosen were encapsulation efficiency, vesicle size, and cumulative drug release. Many methods were used to analyse the microspheres, including X-ray powder diffraction, infrared spectroscopy using the Fourier transform, particle size measurement, and field emissions scanning electron microscopy. The safety and effectiveness of the formulation were also confirmed by in vitro and in vivo drug release experiments. The results showed that the microspheres had a spherical shape with a non-porous surface morphology and a mean particle size of 45±1.23µm. The percentage of encapsulation efficiency ranged from 56±0.82 to 82±0.65, and the percent cumulative drug release ranged from 57±5.6 to 74±4.6. The Eudragit RS-100 polymer demonstrated a sustained drug release profile of up to 14 hours, with higher and longer-lasting anti-inflammatory activity than pure Aceclofenac. The microspheres showed potential in improving patient compliance with minimal or no adverse effects, and their physical appearance and drug content were not affected by accelerated stability testing. Overall, Eudragit RS-100 proved to be an effective sustained-release carrier for developing Aceclofenac-loaded microspheres that enhance efficacy with minimal gastrointestinal side effects during long-term use.