Enhanced biopharmaceutical effects of tranilast on experimental colitis model with use of self‐micellizing solid dispersion technology
Abstract
ABSTRACT The present study aimed to clarify the applicability of a self‐micellizing solid dispersion of tranilast (SMSD/TL) to the treatment of inflammatory bowel diseases (IBD) using an experimental colitis model. SMSD/TL with several loading amounts ranging from 10 to 50% was prepared using a wet‐milling system. The physicochemical properties of SMSD/TL were evaluated in terms of the dissolution behavior, morphology, and particle size distribution. Animal studies were conducted to evaluate oral bioavailability in rats and anti‐inflammatory effects in a rat model of chemically induced colitis. SMSD/TL with drug loading of 15% (SMSD/TL15) showed enhanced dissolution behavior at pH 1.2, compared with other tested other formulations. After the dispersion of SMSD/TL15 in deionized water, fine micelles formed with an average diameter of 137nm. SMSD/TL15 (10mg‐TL/kg) exhibited about 147‐ and 34‐fold greater value for Cmax and the area under the curve of plasma concentration vs. time than crystalline TL, respectively. Although the anti‐inflammatory effect on the colitis model was very limited in the crystalline TL (2mg/kg) group, inflammatory events, such as myeloperoxidase activity and thickening of the submucosa in colon tissues, were significantly suppressed in the SMSD/TL15 (2mg‐TL/kg) group. Based on these findings, SMSD/TL might be a more efficacious dosage option for improved IBD treatment.
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