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A multifunctional folic acid decorated superparamagnetic mesoporous CoFe2O4 based nanocarrier with the particle size of 35–40 nm was synthesized by a simple method. The particles show excellent aqueous dispersion stability in physiological pH without any deterioration in hydrodynamic size and zetapotential. The cytotoxicity and internalization efficiency of these nanocarriers have been evaluated on folate receptor overexpressed HeLa cells. Fluorescent molecule RITC and antitumor agents such as methotrexate and doxorubicin were successfully attached to the surface amine groups following simple organic coupling reactions thus endowing the nanoparticle with therapeutic and optical properties. These drug loaded nanoagents exhibit elevated cytotoxicity and induce apoptosis in HeLa cells.