Development and Characterization of Colon-targeting 5-Fluorouracil Multiparticulate Beads

Abstract

This investigation is related to the development and optimization of multiparticulate beads of fenugreek seed mucilage-sodium alginate containing 5-flurouracil through ionotropic gelation technique using 3 2 full factorial design generated with Design-Expert® Version11 software. The beads were developed using CaCl 2 as the crosslinking agent. The effect of ratio of fenugreek seed mucilage and sodium alginate blend and concentration of CaCl 2 on the drug encapsulation efficiency, bead size and percent cumulative drug release in 6 h was optimized by 3 2 factorial design. The beads were also characterized using field emission scanning electron microscopy, Fourier-transform infrared spectroscopy and thermal analysis. The percent drug encapsulation efficiency of all these beads was within the range of 43.91 to 85.39 % with an in vitro drug release of 33.92 to 39.23 % in 6 h. The optimized batches of beads were coated with Eudragit S100 (5, 10 and 15 % w/v) to facilitate colon targeting in a prominent way. The in vitro drug release from the coated beads (P3) in various colonic fluids followed zero-order pattern with erosion mechanism in 18 h. The average size of these beads was within the range of 895 to 1021 µm. The optimized fenugreek seed mucilage-alginate beads containing 5-flurouracil showed significant drug permeability over a prolonged period in an ex vivo permeability study through goat colon. The results indicated successful colon targeting of 5-flurouracil multiparticulate beads developed using polymeric blends containing sodium alginate and fenugreek seed mucilage in an appropriate ratio.