Iron oxide nanoparticle is the most promising nanoparticles (NPs) capable in Drug Delivery and targeting. Iron oxide nanoparticles were synthesized by green synthesis. Galactomannan, when attached to the surface of the nanoparticles, increases the biocompatibility of the nanoparticles. Folic acid (FA) is used as the ligand to target folate receptors, which are found abundant in cancer cells. FeNPs-GM-FA could target cancer cells when used as drug carriers. The synthesized iron oxide nanoparticles using Mimosa pudica root extract was synthesized for targeted delivery of the anticancer drug, Capecitabine, by grafting folic acid (FA) onto the iron oxide nanoparticles coated with galactomannan (GM), a polysaccharide present in fenugreek gum. The cytotoxicity profile of the nanoparticles on human epithelial type 2 (HEp-2) cells as measured by standard 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay showed that the particles were nontoxic and may be useful for various in vivo and in vitro biomedical applications. The surface modification by galactomannan and folic acid grafting was confirmed by UV-visible spectroscopy and fourier transforms infrared (FTIR) spectroscopy. The in vitro release profile of capecitabine from FeNPs-GM-FA was characterized by an initial fast release followed by a sustained release phase. The histological investigation evidences the formation of improved liver cell architecture indicating the therapeutic nature of functionalized iron nanoparticles with Capecitabine, confirming a potential option for drug delivery and targeting tumor tissues.