China Science

The purpose of this investigation was to prepare; evaluate the colon-specific microspheres of 5-fluorouracil for the treatment of colon cancer. Core microspheres of alginate were prepared by the modified emulsification method in liquid paraffin; by cross-linking with calcium chloride. The core microspheres were coated with Eudragit S-100 by the solvent evaporation technique to prevent drug release in the stomach; small intestine. The microspheres were characterized by shape, size, surface morphology, size distribution, incorporation efficiency,; in vitro drug release studies. The outer surfaces of the core; coated microspheres, which were spherical in shape, were rough; smooth, respectively. The size of the core microspheres ranged from 22 to 55 ?m,; the size of the coated microspheres ranged from 103 to 185 ?m. The core microspheres sustained the drug release for 10 hours. The release studies of coated microspheres were performed in a pH progression medium mimicking the conditions of the gastrointestinal tract. Release was sustained for up to 20 hours in formulations with core microspheres to a Eudragit S-100 coat ratio of 1?7,; there were no changes in the size, shape, drug content, differential scanning calorimetry thermogram,; in vitro drug release after storage at 40°C/75% relative humidity for 6 months.

Ziyaur Rahman1Email:ziyaur_rahman2@rediffmail.com?Kanchan Kohli1?Roop K. Khar1?Mushir Ali1?Naseem A. Charoo1?Areeg A. A. Shamsher1
[1] Department of Pharmaceutics, F/O Pharmacy, Hamdard University, 110063 New Delhi, India ;[2] D-615. Gali No 1, Chauhan Bangar, 110053 Delhi, India