The anti-tumor efficiency of poly(L-glutamic acid) dendrimers with polyhedral oligomeric silsesquioxane cores
作者：Yuji Pu, Shuang Chang, Hui Yuan, Gang Wang, Bin He*, Zhongwei Gu*
關(guān)鍵字：poly(L-glutamic acid) , pH-sensitive
論文來(lái)源：期刊
具體來(lái)源：Biomaterials 2013, 34: 3658-3666
發(fā)表時(shí)間：2013年
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$HCl. The in vivo experiments were carried out in mice xerograft breast cancer models, the results indicated that the inhibition efficiency of the DOX-dendrimer conjugates was much better than that of free DOX$HCl.