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Cationic polymers such as branched poly(ethylenimine) (PEI) have been well-studied due to their superior gene transfection effecacies.However, high toxicity of PEI is a main concern in its clinical application.In our research, we successfully prepared micellar nanoparticles assembled by poly(lactic-co-glycolic acid) (PLGA) as a hydrophobic core packaging a model drug docetaxel inside, PEI as a hydrophilic shell modified with hyaluronic acid(HA) outside binding a specific siRNA suppressing cyclooxygenase-2 (COX-2) gene expression.This novel co-delivery system makes full use of the advantages of siRNA inducing apoptosis at the cellular level as well as anti-cancer activity of the small molecular drug, thus evidently reduces the dosage of the chemical drug and improve administration safety.More importantly, HA conducts the complex to targeted tumor cells expressing CD44 receptors.We evaluated the structural, chemical characteristics, stability, in-vitro drug release behavior of DTX ,cytotoxicity of the carrier, transfection efficacy of the siRNA and in-vivo tumor-target ability.The results showed lower cytotoxicity, higher transfection efficacy and outstanding targeting ability of the co-delivery system.