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Targeted drug delivery coupled with rapid drug release in cytoplasm is a powerful strategy to enhance efficacy and reduce off-target effects of anti-cancer drugs.Herein,we developed a dualfunctional mixed micellar drug delivery system consisting a biocompatible pH-responsive copolymer,D-a-tocopheryl polyethylene glycol 1000-block-poly-(,β-amino ester) (TPGS-b-PBAE or TP) [1],and AS1411 DNA aptamers (Apt) [2] that recognize the over-expressed nucleolin located on plasmamembrane of cancer cells.