Formulation Development, Optimization and Evaluation of Flurbiprofen Microsponge Tablet for the Treatment of...

Area of Science:

• Pharmaceutical Sciences
• Drug Delivery Systems
• Chronopharmaceutics

Background:

• Rheumatoid arthritis (RA) is a chronic autoimmune disease impacting joints, necessitating optimized anti-inflammatory treatments.
• Chronotherapeutics leverages drug release timing to align with disease rhythms, improving efficacy and reducing side effects.
• Flurbiprofen, a non-steroidal anti-inflammatory drug (NSAID), is used for inflammation relief.

Purpose of the Study:

• To develop and optimize Flurbiprofen-loaded microsponges for targeted chronotherapeutic delivery.
• To enhance the therapeutic effect of Flurbiprofen in managing rheumatoid arthritis symptoms.

Main Methods:

• Microsponges were fabricated using the Quasi Emulsion solvent diffusion method.
• Box-Behnken design was employed to optimize variables: PVA concentration, dichloromethane volume, and stirring speed.
• Key parameters analyzed included entrapment efficiency, mean particle size, and 8-hour drug release; in vitro studies compared the optimized formulation with a marketed product.

Main Results:

• The optimized formulation (Batch F-18) exhibited a particle size of 49.12µm, 87.46% entrapment efficiency, and 70.49% drug release at 8 hours.
• These results met acceptance criteria and demonstrated superior performance compared to the marketed Flurbiprofen tablet.
• Microsponge morphology was characterized as porous and spherical.

Conclusions:

• Increased stirring speed reduced particle size and enhanced entrapment efficiency.
• Increased dichloromethane volume led to decreased particle size.
• The optimized Flurbiprofen microsponge formulation shows promise for future in vivo studies and clinical trials in RA management.