Formulation and Evaluation of Flurbiprofen Microsponges Tablet for Effective Treatment of Rheumatoid Arthritis.

Abstract

Introduction: Rheumatoid arthritis (RA) is a chronic, autoimmune and inflammatory disease that mostly impacts the joints.  Chronotherapeutics refers to a treatment method in which in vivo drug availability is timed to match rhythms of disease in order to optimize therapeutic outcomes and minimize side effects. Flurbiprofen is a non-steroidal anti-inflammatory drug, indicated for the relief of inflammation.

Objectives: The aim of the present study was to develop & optimize the microsponges based of Flurbiprofen tablet for Chronotherapeutics for enhanced therapeutic effect.

Methods: Microsponges were developed by quasi emulsion solvent diffusion method. Compatibility of the drug with excipients was studied by FT- IR & DSC Prepared microsponges were  optimized in  order  to analyze the effects of independent variables like concentration  of PVA  (X1), Volume of Dichloromethane ( X2) & stirring speed (X3) on the Entrapment Efficiency (Y1), Mean particle size (Y2) and Drug release at 8 hr (Y3) using box behnken design.  The optimized formulation was subjected to in vitro study. Morphology of obtained microsponges was revealed by scanning electron microscope.

 Result: The F7 was selected as optimized formulation based on particle size of 42.81µm, entrapment efficiency of 88.19%, and drug release at 8 h 64.94%.

Conclusion: The results showed that, as stirring speed increases, the particle size decreases and entrapment efficiency increases. While volume of dichloromethane increases, particle size decreases. Morphology was found to be porous and spherical. Optimized batch of Flurbiprofen microsponge was further formulated as tablet formulation.