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Current Drug Delivery

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ISSN (Print): 1567-2018
ISSN (Online): 1875-5704

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Research Article

QbD-Enabled Systematic Development of Ileo-Colonic Targeted Novel Mucoadhesive Microspheres of Flurbiprofen

Author(s): Saikat Pande*, Janu Vashi and Ajay Solanki

Volume 19, Issue 3, 2022

Published on: 05 January, 2022

Page: [407 - 419] Pages: 13

DOI: 10.2174/1567201818666210708125036

Price: $65

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.

Keywords: Flurbiprofen, colon targeted delivery, chitosan, eudragit L-100, eudragit S-100, quality by design.

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