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A smart zwitterionic oligopeptide liposome (HHG2C18-L) has been demonstrated to have multistage pH-response to mildly acidic tumor extracellular matrix and intracellular compartment for increased cellular uptake,enhanced cytoplasmic distribution and good mitochondrial targeting [1].In order to further improve the in vivo stability and bioavailability,the PEGylated zwitterionic oligopeptide liposome (PEGHG2C18-L) was constructed based on the formulation of HHG2C18-L by decorating it with PEGHG2C18.PEGHG2C18-L also presented high cellular uptake at tumor pH by charge conversion,and efficient mitochondrial targeting effect.