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Optimization of budesonide compression-coated tablets for colonic delivery
Soad A Yehia1, Ahmed H Elshafeey, Ibrahim Sayed
1Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo, Egypt.
AAPS Pharmscitech
|February 10, 2009
Summary
Compression-coated budesonide tablets using pectin demonstrated targeted colonic delivery for inflammatory bowel disease treatment. This formulation significantly reduced inflammation and myeloperoxidase activity in a rabbit colitis model.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Gastroenterology
Background:
- Inflammatory Bowel Disease (IBD) requires targeted drug delivery to the colon.
- Conventional treatments may lack specificity, leading to systemic side effects.
- Budesonide (BUD) is an effective anti-inflammatory corticosteroid for IBD.
Purpose of the Study:
- To formulate budesonide (BUD) compression-coated tablets for colonic-specific delivery.
- To evaluate the therapeutic efficacy of these tablets in an animal model of colitis.
- To compare enzyme-, pH-, and time-dependent polymers for colonic drug release.
Main Methods:
- Formulation of compression-coated tablets using pectin, guar gum, Eudragit, and cellulose acetate butyrate.
- In vitro drug release studies at varying pH (1.2, 6.8, 7.4) and with pectinolytic enzyme.
- In vivo evaluation of therapeutic efficacy in a trinitrobenzenesulfonic acid-induced rabbit colitis model.
Main Results:
- Enzyme-dependent polymers with 75% pectin showed significant release (99.31%) upon pectinolytic enzyme induction.
- pH-dependent Eudragit polymers released 45.58% in the colon.
- Formula F14 (75% pectin) significantly reduced colonic inflammation and myeloperoxidase activity in rabbits.
Conclusions:
- Budesonide compression-coated tablets with 75% pectin offer targeted colonic delivery.
- This formulation demonstrates significant therapeutic benefits in treating experimental colitis.
- Enzyme-dependent delivery systems, particularly using pectin, show promise for IBD management.
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