Basic Study
Copyright ©The Author(s) 2018. Published by Baishideng Publishing Group Inc. All rights reserved.
World J Gastroenterol. Mar 14, 2018; 24(10): 1093-1106
Published online Mar 14, 2018. doi: 10.3748/wjg.v24.i10.1093
Determination of the mitigating effect of colon-specific bioreversible codrugs of mycophenolic acid and aminosugars in an experimental colitis model in Wistar rats
Shakuntala Santosh Chopade, Suneela Sunil Dhaneshwar
Shakuntala Santosh Chopade, Suneela Sunil Dhaneshwar, Department of Pharmaceutical Chemistry, Poona College of Pharmacy, Bharati Vidyapeeth University, Pune 411038, India
Author contributions: Chopade SS and Dhaneshwar SS equally contributed to the conception and design of the study, acquisition, analysis and interpretation of data, drafted the article and made revisions related to the intellectual content of the manuscript.
Supported by Women Scientist Scheme-A (DST), No. SR/WOS-A/LS-1115/2014.
Institutional animal care and use committee statement: All animal experimentation was approved by the Institutional Animal Ethics Committee (IAEC-approval number: CPCSEA/PCH/15/2014-15) of Poona College of Pharmacy, Bharati Vidyapeeth University, Erandwane, Pune 411038, India.
Conflict-of-interest statement: The authors wish to declare no conflict of interest.
Data sharing statement: There are no additional data available in relation to this manuscript.
ARRIVE guidelines statement: The authors have read the ARRIVE guidelines, and the manuscript was prepared and revised according to the guidelines.
Open-Access: This article is an open-access article which was selected by an in-house editor and fully peer-reviewed by external reviewers. It is distributed in accordance with the Creative Commons Attribution Non Commercial (CC BY-NC 4.0) license, which permits others to distribute, remix, adapt, build upon this work non-commercially, and license their derivative works on different terms, provided the original work is properly cited and the use is non-commercial. See:
Correspondence to: Suneela Sunil Dhaneshwar, BPharm, PhD, Professor, Department of Pharmaceutical Chemistry, Poona College of Pharmacy, Bharati Vidyapeeth University, Pune 411038, India.
Telephone: +91-20-25437237 Fax: +91-20-25439382
Received: December 11, 2017
Peer-review started: December 12, 2017
First decision: December 27, 2017
Revised: December 31, 2017
Accepted: January 24, 2018
Article in press: January 24, 2018
Published online: March 14, 2018
Core Tip

Core tip: Mycophenolic acid (MPA), an immunosuppressant and its morpholinoethyl ester prodrug: mycophenolate mofetil are under investigation for the treatment of inflammatory bowel disease (IBD). Diarrhea and local gut toxicity are their major setbacks. The present work focused on the synthesis of colon-targeted prodrugs wherein MPA was bio-reversibly linked with aminosugars to mask the carboxyl group of MPA responsible for gastrointestinal side effects. The synthesized prodrugs exhibited a significant mitigating effect on 2,4,6-trinitrobezenesulfonic acid-induced colitis in Wistar rats compared to MPA. The absence of pancreatitis, hepatitis and the gastro-sparing nature of the prodrugs emphasize their potential which could be investigated further for the management of IBD.