چکیده (انگلیسی):

The purpose of this investigation was to prepare and 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 and 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 and small intestine. The microspheres
were characterized by shape, size, surface morphology,
size distribution, incorporation efficiency, and in vitro drug
release studies. The outer surfaces of the core and coated
microspheres, which were spherical in shape, were rough
and smooth, respectively. The size of the core microspheres
ranged from 22 to 55 μm, and the size of the coated microspheres
ranged from 103 to 185 μm. 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, and there were no changes in the size, shape,
drug content, differential scanning calorimetry thermogram,
and in vitro drug release after storage at 40°C/75% relative
humidity for 6 months.