Related Experiment Video
Updated: May 15, 2025

Investigating the Alleviating Effects of Bacillus cereus Administration on Colitis through Gut Microbiota Modulation
Published on: July 27, 2022
Novel Enteric Microsphere of Beclomethasone Dipropionate With Colon Delivery and Enhancement of Anti-Inflammatory
Atsushi Uchida1,2, Yuto Hayashi1, Tsubasa Kihara1
1Laboratory of Biopharmacy, School of Pharmaceutical Sciences, University of Shizuoka, Suruga-ku, Japan.
Abstract:
The present study aimed to develop a novel colon-targeting microsphere of beclomethasone dipropionate (cMS/BDP) with enhanced pharmacological effect of BDP in the colon. cMS/BDP was prepared using Eudragit® S-100 by the emulsion solvent diffusion method, and its physicochemical properties were characterized. A pharmacokinetic study was conducted to assess systemic exposure and colon distribution of BDP after oral administration of cMS/BDP to rats. A pharmacodynamic study was carried out to evaluate the anti-inflammatory effect of cMS/BDP after its oral administration to ulcerative colitis model rats. The particle size of cMS/BDP was calculated to be ca. 20 μm, and most BDP in cMS/BDP might be in an amorphous state. In dissolution tests, cMS/BDP showed pH-dependent release behavior of BDP and marked BDP release at pH 7.4. After oral administration of cMS/BDP (5 mg-BDP/kg) to rats, BDP was rapidly metabolized to beclomethasone 17-monopropionate (17-BMP, a BDP metabolite) in the gastrointestinal tract and liver, and relative oral bioavailability of 17-BMP in the cMS/BDP group was calculated to be ca. 4.8% compared with that in the BDP solution group. The tissue-to-plasma partition coefficient value, an index of colon distribution, for cMS/BDP was found to be 15-fold higher than that for BDP solution. In the cMS/BDP (50 μg/kg) group, colonic myeloperoxidase activity and hyperplasia of the submucosa were negligibly elevated. From these findings, the cMS approach for BDP would be a promising dosage option for strategic colon delivery, leading to an improved therapeutic potential of BDP with a wide safety margin.
More Related Videos
09:34Uptake of New Lipid-coated Nanoparticles Containing Falcarindiol by Human Mesenchymal Stem Cells
Published on: February 9, 2019
08:58Analyzing Beneficial Effects of Nutritional Supplements on Intestinal Epithelial Barrier Functions During Experimental Colitis
Published on: January 5, 2017
Related Concept Videos
Drugs for Treatment of Crohn's Disease in IBD Using Glucocorticoids
Drugs for Treatment of Ulcerative Colitis in IBD
Drugs for Treatment of Constipation-Predominant IBS
Drugs for Treatment of Crohn's Disease in IBD Using Immunomodulatory Agents
Drugs for Treatment of Diarrhea-Predominant IBS
Two specific drugs used in the treatment are alosetron (Lotronex) and eluxadoline (Viberzi). Alosetron, a 5-HT3 antagonist, works by slowing the movement of stools in the gut, reducing bowel...
Drug Delivery: Miscellaneous Routes
Oral inhalation and nasal sprays swiftly transfer drugs across the respiratory epithelium's mucosal layer. Inhaled glucocorticoids and bronchodilators directly target lung conditions such as asthma, while fluticasone nasal spray mitigates allergic rhinitis.
Transdermal patches transport drugs...