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World J Gastroenterol. Apr 7, 2014; 20(13): 3564-3571
Published online Apr 7, 2014. doi: 10.3748/wjg.v20.i13.3564
Published online Apr 7, 2014. doi: 10.3748/wjg.v20.i13.3564
Colon-specific prodrugs of 4-aminosalicylic acid for inflammatory bowel disease
Suneela S Dhaneshwar, Department of Pharmaceutical Chemistry, Poona College of Pharmacy, Bharati Vidyapeeth Deemed University, Pune-411 038, Maharashtra, India
Author contributions: Dhaneshwar SS has conceptualized, drafted and compiled this comprehensive review through extensive survey of the available literature and databases, adding a new perspective based on her expertise in this area.
Correspondence to: Suneela S Dhaneshwar, M. Pharm, PhD, Professor of Pharmaceutical Chemistry, Department of Pharmaceutical Chemistry, Poona College of Pharmacy, Bharati Vidyapeeth Deemed University, Bharati Vidyapeeth Campus, Pune-411 038, Maharashtra, India. suneeladhaneshwar@rediffmail.com
Telephone: +91-20-25437237 Fax: +91-20-25439383
Received: October 31, 2013
Revised: December 17, 2013
Accepted: January 8, 2014
Published online: April 7, 2014
Processing time: 154 Days and 20.4 Hours
Revised: December 17, 2013
Accepted: January 8, 2014
Published online: April 7, 2014
Processing time: 154 Days and 20.4 Hours
Core Tip
Core tip: Anti-inflammatory activity of antitubercular drug 4-aminosalicylic acid (ASA) was first described by Lover in 1984. Since then, numerous clinical trials were carried out to establish its efficacy in left-sided and active/quiescent ulcerative colitis. It is 50% more potent than 5-ASA against inflammation and does not produce 5-ASA-induced immunoallergic acute pancreatitis. 4-ASA is a stable and inexpensive alternative to 5-ASA in patients with acute pancreatitis. Despite all these positive findings, an extensive literature review surprisingly revealed few colon-targeting delivery systems for 4-ASA. The present review presents a complete profile of 4-ASA and its colon-specific prodrugs for inflammatory bowel disease.