Title:QbD-Enabled Systematic Development of Ileo-Colonic Targeted Novel Mucoadhesive Microspheres of Flurbiprofen
Volume: 19
Issue: 3
Author(s): Saikat Pande*, Janu Vashi and Ajay Solanki
Affiliation:
- Department of Pharmaceutics, A. R. College of Pharmacy and G.H. Patel Institute of Pharmacy, Vallabh Vidyanagar,
Anand, India
Keywords:
Flurbiprofen, colon targeted delivery, chitosan, eudragit L-100, eudragit S-100, quality by design.
Abstract: Background: Flurbiprofen (FLBP), used in the treatment of ulcerative colitis, 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 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 were coated successfully with different
ratios of Eudragit L-100 to Eudragit S-100. The release profile of the optimized batch matches
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 as
a suitable for delivering FLBP to the Ileo-colonic region of the GIT in the treatment of ulcerative
colitis.
