TARAK J. MEHTA, SATYANARAYAN SINGH RAJPUT, MUKESH R. PATEL, KANU R.PATEL NATVARLAL M. PATEL, MOHAN MOTHILAL
The Oral controlled - release formulations for the small intestine and colon have received considerable attention in the past 25 years for a variety of reasons including pharmaceutical superiority and clinical benefits derived from the drug - release pattern that are not achieved with traditional immediate (or) sustained - release products Although 5-FU is a widely used antineoplastic agent, the cytotoxicity is not limited to tumor cells. Hematopoietic cells and normal epithelial cells of GI tract are susceptible to 5-FU induced cytotoxicity, which produces sever leucopenia and intestinal toxicity leading to lethal translocation of intestinal microflora. The clinical use of 5-FU is limited by its GI toxicity (stomatitis) and myelotoxicity1, and oral bioavailability was found to be only 28% in humans. On other hand, severe systemic toxic effects and shorter half life make this drug particularly suitable to be delivered by local delivery system providing continuously sustained release1. Targeted delivery of 5- FU not only reduces systemic side effects, but also would provide an effective and safe therapy for colon cancer with reduced dose and duration of therapy.
