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It is a potential strategy to increase the selectivity of cell penetrating peptide (CPP) to tumor by the regulation of PEG-Hz-DSPE on the surface of liposomes.In this work, we developed an efficient PEGylated liposomal nanocarrier (CPPL) containing CPP and pH-sensitive hydrazone bond to enhance doxorubicin (DOX) tumor-targeted delivery in vivo.