Abstract
Purpose: The main objective of the present study was to develop the colonic delivery system for 5-aminosalicylic acid (5-ASA) as an anti-inflammatory drug. Methods: Matrix pellets containing various proportions of alginate, calcium and Eudragit® RS were prepared by extrusion-spheronization technique. Thermal treatment was used to investigate the effect of the curing process on the surface morphology, mechanical and physicochemical properties and in vitro drug release profile of pellets. Based on the obtained results optimal formulations were selected to coating by the Eudragit® RS and subjected to a subsequent continuous dissolution test. Results: Image analysis and also scanning electron microscopy results proved acceptable morphology of the pellets. The fourier transform infrared spectroscopy and differential scanning calorimetry studies ruled out any interactions between the formulation’s components. Curing process did not alter the mechanical properties of pellets. The release rate of the drug from matrices was prolonged due to the decreased porosity of cured pellets. Furthermore, selected cured pellets which coated with Eudragit® RS, prevented undesired premature drug release. Conclusion: Formulation containing 17.5% calcium, 17.5% alginate, and a coating level of 10% demonstrated enhanced drug release so that provided resistance to acidic conditions, allowing complete drug release in alkaline pH, mimicking colonic environment. The slow and consistent drug release from this formulation could be used for treatment of a broader range of Inflammatory bowel disease (IBD) patients especially in whom colonic pH levels have been measured at lower than pH 7.0.
Highlights
Inflammatory bowel disease (IBD), which caused the inflammation of the gastrointestinal tract (GIT), consists of two groups, including Crohn’s disease and ulcerative colitis
Thermal treatment was used to investigate the effect of the curing process on the surface morphology, mechanical and physicochemical properties and in vitro drug release profile of pellets
Image analysis results showed that the sphericity of the most formulations was higher than 0.7, which indicates that the pellets are almost spherical
Summary
Inflammatory bowel disease (IBD), which caused the inflammation of the gastrointestinal tract (GIT), consists of two groups, including Crohn’s disease and ulcerative colitis. GIT is the main site of pathology in IBD patients, so the oral route has the potential to deliver the drug to the site of action.[1] Corticosteroids are potent antiinflammatory therapies, but their long-term use is often caused severe systemic side effects such as hypertension, hyperglycemia, and immunosuppression.[2] 5-aminosalicylic acid (5-ASA) is still considered as firstline therapy for mild to moderate types of IBD. Optimizing the drug delivery systems is necessary for avoiding the systemic side effects as well as improving the local bioavailability of 5-ASA at target inflamed tissues. Until now, a wide range of oral colon targeted drug delivery systems have been investigated. Matrix drug delivery systems include hydrophobic and hydrophilic types. Hydrophilic matrices are widely used for sustained drug release in GIT. The swelling and eroding behavior of these matrices in an aqueous medium provides the potential to acquire a suitable dissolution profile.[6]
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