Development, optimization and evaluation of colon targeted drug delivery system utilizing 22 factorial design using ibuprofen as model dr

Abstract

Colon-specific drug delivery systems (CDDS) are not only desirable for the treatment of a range of local diseases such as ulcerative colitis, Crohn’s disease, irritable bowel syndrome, chronic pancreatitis, and colonic cancer but also systemic delivery of proteins and peptides this is because of less diversity and intensity of digestive enzymes and less proteolytic activity of colon mucosa than that observed in the small intestine. The purpose of the present investigation was to prepare matrix tablets using polymers such as guar gum and pectin and the tablets were further coated with different concentrations of Eudragit S-100, a pH-sensitive polymer, by dip immerse method. In vitro drug release investigations of tablets were done in various dissolution media, i.e., 0.1 N HCl (pH 1.2), phosphate buffers pH 7.4, with or without rat cecal content. The swelling studies of all formulations were carried out. The physicochemical parameters of the formulations were seen as in consistence with the pharmacopoeial standards for pre and post compression evaluations. The stability studies for all formulations were executed according to ICH guideline and the result showed less degradation during accelerated and room temperature storage conditions for 6 months. The result of drug release study demonstrated that the tablets coated with Eudragit S-100 (30% w/v) showed a sustained release of 93.4% for 13 h, while the uncoated tablets released the drug within 5 h. With regard to release kinetics, the data were best fitted with the Hixson Crowell model. Thus the enteric-coated Eudragit S-100 coated matrix tablets of ibuprofen showed promising site-specific drug delivery in the colon region.