title: Preparation and evaluation of mesalamine collagen in situ rectal gel: a novel therapeutic approach for treating ulcerative colitis.
abstract: Ulcerative colitis (UC) is a chronic inflammatory disease that primarily affects the colonic mucosa. Mesalamine had been established as a first line drug for treating mild to moderate UC. A continued availability of the drug for treatment of damaged tissues remains a great challenge today. In the present study, a novel mesalamine collagen in situ gel has been prepared using type I collagen, which is pH/temperature sensitive. This hydrogel undergoes sol-gel transition under physiological pH and temperature which was confirmed by rheological studies. The in vitro release profile demonstrated sustained release of mesalamine over a period of 12h. The in vivo efficacy of the in situ gel was performed using dextran sodium sulphate induced ulcerative colitis model in BALB/c mice. The clinical parameters such as, body weight changes, rectal bleeding and stool consistency were evaluated. In addition, the histopathological investigation was conducted to assess severity of mucosal damage and inflammation infiltrate. There was a significant reduction in rectal bleeding and mucosal damage score for collagen-mesalamine in situ gel group compared to the reference group. Apart from releasing mesalamine in controlled manner, the strategy of administering mesalamine through collagen in situ gel facilitates regeneration of damaged mucosa resulting in a synergistic effect for the treatment of ulcerative colitis.
authors.affiliation: Central Leather Research Institute, Council of Scientific and Industrial Research, Adyar, Chennai 600 020, Tamil Nadu, India.
authors.forename: Satiesh Kumar
authors.initials: SK
authors.lastname: Ramadass
authors.forename: Sathiamurthi
authors.initials: S
authors.lastname: Perumal
authors.forename: Sugin Lal
authors.initials: SL
authors.lastname: Jabaris
authors.forename: Balaraman
authors.initials: B
authors.lastname: Madhan
mesh_terms: D000285:Administration, Rectal; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage* / Q000737:chemistry; D003093:Colitis, Ulcerative / Q000139:chemically induced / Q000188:drug therapy* / Q000473:pathology; D024042:Collagen Type I / Q000008:administration & dosage* / Q000737:chemistry; D016264:Dextran Sulfate; D004339:Drug Compounding; D005260:Female; D005782:Gels; D006863:Hydrogen-Ion Concentration; D019804:Mesalamine / Q000008:administration & dosage* / Q000737:chemistry; D051379:Mice; D008807:Mice, Inbred BALB C; D013696:Temperature
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D024042:Collagen Type I; D005782:Gels; D019804:Mesalamine; D016264:Dextran Sulfate