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Peptide dendrimers represent superior drug carriers for their unique nanoarchitectures, excellent degradability and biocompatibility. In this research, poly(L-glutamic acid) dendrimers with polyhedral oligomeric silsesquioxane (POSS) as cores were synthesized. Tumor targeting moiety (biotin) and therapeutic drug doxorubicin (DOX) were immobilized on the dendrimers via pH-sensitive hydrazone bonds. The size distribution and morphology of the drug-dendrimer conjugates were characterized by DLS, AFM, and TEM. The drug release profiles, cellular uptake, in vitro and in vivo anti-tumor activities of the conjugates were investigated. The results revealed that the conjugates aggregated nanoparticles with the size around 100 nm. The drug-dendrimer conjugates could be internalized in mice breast cancer 4T1 cells efficiently. The IC₅₀ of the conjugates was comparable to that of DOX·HCl. The in vivo experiments …