The present investigation is aimed to develop a new formulation containing chemically crosslinked
guar gum microspheres loaded with
5-fluorouracil for targeting
colorectal cancer. The emulsification polymerization method involving the dispersion of aqueous phase of
guar gum in
castor oil was used to prepare spherical
microspheres. Various processing parameters were studied in order to optimize the formulation. Particle size and surface morphology of the
microspheres were determined using optical microscopy and scanning electron microscopy. The in vitro drug release studies performed in simulated gastric fluid (SGF) for 2 h followed by intestinal fluid for 3 h, revealed the retention of the
drug inside the
microspheres from which only (15.27 +/- 0.56) % of the
drug was released in 5 h. In vitro release rate studies were also carried out in simulated colonic fluid (SCF) in the presence of rat caecal contents, which showed improved drug release. The drug release from the formulation was found to be (41.6 +/- 3.5) % with 2% (w/v) caecal matter in 24 h as compared to control study where (25.2 +/- 3.5) % of
drug was released. The drug release from the formulation with 2% and 4% rat caecal contents medium after 2 days of enzyme induction was found to be (56.3 +/- 4.1) % and (78.9 +/- 2.8) % in 24 h respectively. Similarly, (61.3 +/- 5.4) % and (90.2 +/- 2.9) %
drug was released respectively with 2% and 4% rat caecal matter after 4 days of enzyme induction and (72.1 +/- 2.9) % and (90.2 +/- 3.2) % after 6 days of enzyme induction. In this way,
5-fluorouracil loaded
guar gum microspheres have shown promising results in the management of
colorectal cancer, warranting thorough in vivo study for scale up technology.