Synthesis and evaluation of a novel cancer cell’s receptor-targeted internally quaternized and surface neutral poly(amidoamine) (PAMAM) generation four dendrimer as well as PAMAM–paclitaxel conjugate are described. The advantages of developed nanocarriers include but are not limited to (1) internal cationic charges for the complexation with small interfering RNA or antisense oligonucleotides and their protection from the degradation in systemic circulation; (2) neutral-modified surface for low cytotoxicity of empty unloaded dendrimers; (3) efficient internalization by cancer cells; and (4) preferential accumulation in the tumor and the prevention of adverse side effects of chemotherapy.
