In our current study, a newer
amine functionalized
guar gum derivative was studied for its efficacy in colonic
drug delivery.
Glycyrrhizic acid mono-
ammonium salt was used as the model
drug.
Drug-loaded microparticles were formulated by ionic crosslinking using
sodium tripolyphosphate. The Scanning Electron Microscopic study revealed spherical particles of sizes from 4.9 ± 3.8 μm to 6.9 ± 3.9 μm. The FT-IR studies presented a possible interaction between the
drug and the
polymer. The
drug was encapsulated in amorphous form as observed from the
powder X-Ray Diffraction studies. A cumulative drug release study was carried out in simulated gastric, intestinal, and colonic fluids. The cumulative drug release studies presented a burst release followed by a sustained release of the
drug in simulated colonic fluid containing rat cecal contents. The
drug-
polymer ratio was optimised using a 3(2) factorial design by taking the amounts of
glycyrrhizic acid (X1) and
guar gum alkyl
amine (X2) as the independant variables. The percent cumulative drug release at 240 mins (Q240), 720 mins (Q720), and at 1,440 mins (Q1440) were considered as the dependant variables. The efficacy of the optimized formulation was studied in a
2,4,6-trinitrobenzene sulfonic acid-induced rat
colitis model. The tissue's
nitric oxide,
malondialdehyde, and
myeloperoxidase activities were found to be much lower in the microparticle-treated group compared to free
drug-treated group. The histology of the colonic tissue from the treated group of animals revealed almost no infiltration of inflammatory cells in the tissue for the microparticle-treated group of animals. The synthesized
amine derivative of
guar gum was found to be better in vitro with a better in vivo efficacy in the colonic delivery of
glycyrrhizic acid monoammonium
salt and can be considered as a newer modified
biopolymer for colonic
drug delivery.