Chopade SS, Dhaneshwar SS. Determination of the mitigating effect of colon-specific bioreversible codrugs of mycophenolic acid and aminosugars in an experimental colitis model in Wistar rats. World J Gastroenterol 2018; 24(10): 1093-1106 [PMID: 29563754 DOI: 10.3748/wjg.v24.i10.1093]
Corresponding Author of This Article
Suneela Sunil Dhaneshwar, BPharm, PhD, Professor, Department of Pharmaceutical Chemistry, Poona College of Pharmacy, Bharati Vidyapeeth University, Pune 411038, India. suneeladhaneshwar@rediffmail.com
Research Domain of This Article
Gastroenterology & Hepatology
Article-Type of This Article
Basic Study
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Chopade SS, Dhaneshwar SS. Determination of the mitigating effect of colon-specific bioreversible codrugs of mycophenolic acid and aminosugars in an experimental colitis model in Wistar rats. World J Gastroenterol 2018; 24(10): 1093-1106 [PMID: 29563754 DOI: 10.3748/wjg.v24.i10.1093]
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, 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.
Correspondence to: Suneela Sunil Dhaneshwar, BPharm, PhD, Professor, Department of Pharmaceutical Chemistry, Poona College of Pharmacy, Bharati Vidyapeeth University, Pune 411038, India. suneeladhaneshwar@rediffmail.com
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 Processing time: 91 Days and 19.2 Hours
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.
