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Investigation of mitigating effect of colon-specific prodrugs of boswellic acid on 2,4,6-trinitrobenzene sulfonic acidinduced colitis in Wistar rats: Design, kinetics and biological evaluation

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World Journal of Gastroenterology 2017年第7期23卷 1147-1162页

作者： Ajinkya Sarkate Suneela S Dhaneshwar Department of Pharmaceutical Chemistry Poona College of PharmacyBharati Vidyapeeth UniversityMaharashtra 411038India

AIM To develop a colon-targeting bioreversible delivery system for β-boswellic acid(BBA) and explore utility of its prodrugs in 2,4,6-trinitrobenzene sulfonic acid(TNBS)-induced colitis in *** Synthesis of 4 co-drugs of BBA with essential amino acids was achieved by CDI coupling, followed by their spectral characterization. In vitro kinetics were studied by HPLC in aqueous buffers, homogenates of gastrointestinal tract and fecal matter. In vivo kinetic studies were performed in Wistar rat plasma, urine and feces. The prodrugs were screened in TNBS-induced colitis modeled Wistar rats. Statistical significance was assumed at P prodrugs were stable in 0.05 mol/L HCl buffer(p H 1.2) and stomach homogenates. Negligible hydrolysis was observed in phosphate buffer and intestinal homogenates. Substantial release(55%-72% and 68%-86%) of BBA was achieved in rat fecal matter and homogenates of colon. In vivo studies of BBA with L-tryptophan(BT) authenticated colon-specific release of BBA. But, surprisingly substantial concentration of BBA was seen to reach the systemic circulation due to probable absorption through colonic mucosa. Sitespecifically enhanced bioavailability of BBA could be achieved in colon, which resulted in demonstration of significant mitigating effect on TNBS-induced colitis in rats without inducing any adverse effects on stomach, liver and pancreas. Prodrug of BT was found to be 1.7%(P prodrugs tested. CONCLUSION The outcome of this study strongly suggests that these prodrugs might have dual applicability to inflammatory bowel disease and chronotherapy of rheumatoid arthritis.

关键词：煽动性的肠疾病 Boswellic 酸互补、其他的药指向冒号相互的 prodrugs 氨基酸导致 TNBS 的大肠炎

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