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A mixed micellar system based mainly on the pH-sensitive copolymer of poly (L-histidine)-poly (D,L-lactide)-polyethyleneglycol- poly (D,L-lactide)-poly (L-histidine) (PHis-PLA-PEG-PLA-PHis) and Pluronic(R) F127,some of which was conjugated with folate,was constructed to intracellularly deliver the unimers of Pluronic(R) P85 to MDR cells.The micelles with inserted Pluronic(R) P85 unimers demonstrated much more cellular uptake and higher cytotoxicity against MDR cells than other tested formulations.The enhanced MDR reversal effect was attributed to the intracellular delivery of Pluronic(R) P85 unimers to the MDR cells.The intracellular delivery of Pluronic(R) P85 unimers to the MDR cells has been demonstrated as a promising approach to reverse MDR.