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The success of anti-cancer drug targeting is depends on the ability of the therapeutics to reach their desirable cellular and intracellular sites and minimizing action at the nonspecific sites. In the present study, anti-human epidermal growth factor receptor (HER-2, ErbB2) antibody anchored nanoparticles were prepared and evaluated for the assessment of targeting potential in breast cancer cell. In an attempt for comparison of carrier system for site-selective delivery, docetaxel loaded PLGA nanoparticles, PLGA-PEG nanoparticles and PLGA-PEG immunonanoparticles capable of targeting breast cancer were prepared by emulsion solvent evaporation technique. The drug-loaded nanoparticles were characterized for their size and size distribution, surface charge, drug encapsulation efficiency and in vitro drug release. Our results demonstrate that docetaxel loaded PLGA-PEG immunonanoparticles strongly enhances the site specific uptake and high cytotoxic effect at targeted sites, as compared with PLGA, PLGA-PEG nanoparticles. In conclusion polymeric immunonanoparticles could be a promising carrier for the treatment of HER2-overexpressing breast cancers.