In this research, the anti-cancer efficacy of oxaliplatin (OX) was modulated using a nanocarrier system with enhanced targeting efficacy towards folic acid receptors (FAR) expressing colorectal cancer cells. Oxaliplatin was loaded into polyamidoamine dendrimers G4 (PAMAM) imprinted with polyethylene glycol (PEG) and folic acid (FA). The nano-complexes were characterized by FT-IR, 1 H NMR, DSC, TGA, SEM, TEM, DLS and Zeta potential analyzer. Drug loading efficiency (34%) and in vitro drug release studies of PEG-PAMAM-FA-OX nano-complex showed higher drug release at acidic pH. Furthermore, in vitro investigation of nano-complex was carried out using cellular uptake (84.67 +/- 1.98% for colorectal cancer cell line), MIT assay, flow cytometry assay and acridine orange staining, to ascertain the cell internalization efficiency, cell viability, apoptotic phase and morphology of dead cell, respectively. Less value of cell viability (18.39 +/- 1.91%) and more value of late apoptotic phase (81.8%) were obtained for PEG-PAMAM-FA-OX nano-complex as a final synthetic system.