To make significant progress in the fight against cancer, treatment should target cells more specifically, produce fewer side effects, be easy to administer and deter tumor viability on multiple levels. We have attained dramatic in vivo tumor shrinkage and tumor vasculature disruption using a ternary biomolecular nanoparticle comprised of polymeric carrier polysaccharide heparin, anticancer drug retinoid and targeting ligand folic acid. The conjugation of retinoid and folic acid to heparin enhanced the water solubility of the drug, enabled selective targeting, and enhanced the role of heparin as anti-cancer drug carrier by eluding the coagulation cascade. This approach for targeting tumor holds great promise for treatment of various types of cancer. The folic acid linked heparin-retinoid conjugates (HFR) reactions was conjugated with ester and amide bonding which was confirmed by fourier transform infrared (FT-IR) and proton nuclear magnetic resonance (1H-NMR). The ratio of HFR conjugates was measured with Ultra-Violet spectrometry (UV-spectrometry). The particle size of HFR nanoparticles was measured by dynamic light scattering (DLS), and transmission electron microscopy (TEM). HFR conjugates were spherical and showed a diameter range of 200-300 nm in size. The nanoparticles maintained their stability in serum condition for 48hrs and have the high potential for applications in biomedical field.