5-Fluorouracil loaded Eudragit RL 100 and RS 100
Microsponges for Colonic Targeting
Mahmoud Hassan1, Gamal Zayed1 , Osama Farghaly2 and Ahmed A. H. Abdellatif1
1
Faculty of Pharmacy, Department of Pharmaceutics and Industrial pharmacy, Al-Azhar
University, Assuit, Egypt.
2
Faculty of Pharmacy, Department of Pharmaceutics, Minia University, Minia, Egypt.
Abstract
In the present study, eudrgit RL100 and RS100 microsponges (MS) loaded with 5Fluorouracil (5-FU) were prepared by the oil in oil emulsion solvent diffusion method using
acetone as dispersing solvent and liquid paraffin as the continuous medium. MS-5-FU was
designed as novel colon specific drug delivery system for 5-FU, a pyrimidine analog, is
widely used in the treatment of cancers. Process parameters were analyzed in order to
optimize the MS-5-FU formulations. The effects of drug:polymer ratio, the effect of
magnesium stearate concentration and acetone volume on the physical characteristics of MS
were investigated. Shape and surface morphology were examined using scanning electron
microscope. Yield production, encapsulation efficiency and particle size of MS was also
investigated. The results indicate successful preparation of MS; all prepared MS were
spherical in shape with several pores on their surfaces. For MS prepared using Eudragit RL
100, production yield was in the range of (78.7 % and 99.8 %), encapsulation efficiency was
in the range of (65.88 % and 98.7 %) and particle size was in the range of (15.9 µm and 30.04
µm). For MS prepared using eudragit RS 100, production yield was the range of (62.76 %
and 93.8 %), encapsulation efficiency was in the range of (71.8 % and 101.9 %) and particle
size was (10.4 µm and 26.4 µm). This study presents a new approach based on MS for colon
specific drug delivery.