Design and Evaluation of Colon Targeted Dosage Form Containing Mesalazine Using pH Dependent Polymers

Abstract

Colonic drug delivery has gained importance not just for the delivery of the drugs for the treatment of local diseases associated with the colon like Crohn’s disease, ulcerative colitis and irritable bowel syndrome but also for the potential it holds for the systemic delivery of proteins and therapeutic peptides. The aim of the study was to develop colon targeted tablets of Mesalazine by wet granulation method using 33 response surface method with design of experiment software and HPMC K4M, Eudragit RL100, Ethyl cellulose and PVP K-30 used as pH dependent polymers. All the formulations (F1 to F27) were evaluated for the physicochemical parameters and were subjected to in vitro drug release studies. The amount of Mesalazine released from tablets at different time intervals was estimated by UV spectrophotometer. The formulation F26 released 98.16% of Mesalazine after 24 h. The results of the study showed that formulation F26 is the best formulation based on the evaluation parameters which provides targeting of Mesalazine for local action in the colon owing to its minimal release of the drug in the first 4 h. The pH dependent tablet system is a promising vehicle for preventing rapid hydrolysis in gastric environment and improving oral bioavailability of Mesalazine for the treatment of disease at colon region.