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 32 full factorial design generated with Design-Expert® Version11 software. The beads were developed using CaCl2 as the crosslinking agent. The effect of ratio of fenugreek seed mucilage and sodium alginate blend and concentration of CaCl2 on the drug encapsulation efficiency, bead size and percent cumulative drug release in 6 h was optimized by 32 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.