Saikat Pande*, Janu Vashi and Ajay Solanki
Background: Flurbiprofen (FLBP) is used in the treatment of ulcerative colitis and has a short biological half-life. Frequent intake of FLBP may lead to some serious gastric complications, which makes FLBP an ideal candidate for sustained release preparation to the Ileo-colonic region of the gastrointestinal tract (GIT).
Objective: The objective of this study was to investigate the potential of Eudragit coated chitosan microspheres in delivering Flurbiprofen in a sustained manner to the Ileo-colonic region of the GIT for treatment of ulcerative colitis.
Methods: In the present study, mucoadhesive chitosan microspheres were prepared using the emulsion solvent evaporation method by varying different process parameters. Optimized chitosan microspheres were coated with Eudragit L-100 and Eudragit S-100. A 32 full factorial design was applied for optimization. The effect of independent variables (Eudragit L-100 to Eudragit S-100 ratio and stirring speed) on the dependent variable, i.e., percentage cumulative drug release (%CDR) at 3 h and 24 h was evaluated. The optimized batch was evaluated by FT-IR, DSC study, XRD study, and SEM analysis.
Results: Discrete spherical shape chitosan microspheres with entrapment efficiency of up to 95.4% were obtained and selected for coating. Chitosan microspheres coated successfully with different ratios of Eudragit L-100 to Eudragit S-100. The release profile of the optimized batch match with the desired release profile. FLBP was found to be stable and molecularly dispersed in the polymer matrix.
Conclusion: Taken together, it can be concluded that prepared microspheres may be considered suitable for delivering FLBP to the Ileo-colonic region of the GIT in the treatment of ulcerative colitis.
Flurbiprofen, colon targeted delivery, chitosan, Eudragit L-100, Eudragit S-100, Quality by Design
Department of Pharmaceutics, A. R. College of Pharmacy and G. H. Patel Institute of Pharmacy, Vallabh Vidyanagar, Anand, Department of Pharmaceutics, A. R. College of Pharmacy and G. H. Patel Institute of Pharmacy, Vallabh Vidyanagar, Anand, Department of Pharmaceutics, A. R. College of Pharmacy and G. H. Patel Institute of Pharmacy, Vallabh Vidyanagar, Anand