Formulation and Evaluation of Drugs by using Colon Specific Drug Delivery System

Abstract

The prevalence of inflammatory bowel disease (CD and UC) serious colonic disorder has been on the rise throughout the world. Patients suffering from IBD experience poor quality of life with constant remissions and painful exacerbations of disease throughout their lifetime. IBD is a lifelong, relapsing, inflammatory disorder for which patients seek medical therapy in order to progress symptoms and decrease the risk of progression, complications and surgery. Conventional treatments have been only partially successful in treating IBD. Various approaches have been studied for colonic drug delivery but each aspect has shown some disadvantages. Currently in the market there is no immediate release Mesalamine formulation to target ileo-cecal region and Budesonide formulation for colonic delivery to treatment of IBD. Therefore it was planned to develop such formulation which will release drug in the ileo-cecal region and proximal colon based pulsatile and sustained release, pH dependant polymer coated pellets respectively that allowed drug release and absorption after a lag time of about 4 to 5h to treat mild to moderate CD and UC. newlineThe present study directed to formulate, optimize and evaluate a multiparticulate system for efficient CSDDS in two parts. Mesalamine and Budesonide are used as model drugs. Mesalamine is an anti-inflammatory agent and is an established treatment for IBD. Studies have shown that mesalamine therapy is only moderately superior and successful in inducing symptomatic condition. Budesonide is a potent, synthetic non-halogenated corticosteroid with high topical anti-inflammatory effect. First part deals with Mesalamine burst release pellets coated with Croscarmellose sodium and Eudragit S100 for ileocecal targeting to treat mild to moderate CD and second part deals with Budesonide sustained release pellets coated with HPMC K100M and Eudragit S100 for potential colonic delivery to treat mild to moderate UC and for maintenance therapy during disease remission. newline newline