DEVELOPMENT OF DUAL MATRIX BASED COLON TARGETED DELAYED RELEASE BUDESONIDE TABLETS FOR THE TREATMENT OF INFLAMMATORY BOWEL DISEASES

Abstract

Current work was aimed to develop and assess colon-targeted delayed release dual matrix formulations and microcapsules of anti-inflammatory drugs Budesonide and Mesalamine as a novel avenue for the treatment of inflammatory bowel diseases. Eight different dual matrix core tablet formulations (B1-B8) containing 9 mg of Budesonide were prepared using different concentration of Eudragit® L100, PolyoxTM WSR303 and Carbopol® 971 based on factorial design with three factors and two levels (23). Coating the prepared matrix core was done with a 10% w/w Eudragit® L30D solution. The developed formulations were tested for product attributes like weight variation, thickness/ hardness, percent friability, content-uniformity, swelling index, mucoadhesion strength, and in-vitro drug dissolution in dissolution media simulating gastrointestinal conditions. Studies of the stability and in-vitro release kinetics of the tablets were also conducted. IR spectral analysis shows that a drug and polymer physical mixture was safe and did not react chemically with one another. All Budesonide tablet formulations (B1–B8) with a dual matrix had pre-compression values that were within the allowed range. Tablet thickness, weight fluctuation, friability, and content uniformity were all within acceptable ranges after compression, as defined by the Pharmacopeia. Formulation B5 (100 mg of Eudragit® L100 and 120 mg of PolyoxTM WSR303 was shown to have the highest tablet swelling index and mucoadhesive strength. Stability experiments confirmed that formulation B5 was stable and that it provided the best in-vitro drug release.