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Conjugation of Iron Oxide Nanoparticles with RGD-Modified Dendrimers for Targeted Tumor MR Imaging

Yang, Jia, Luo, Yu, Xu, Yanhong, Li, Jingchao, Zhang, Zaixian, Wang, Han, Shen, Mingwu, Shi, Xiangyang, Zhang, Guixiang
ACS Applied Materials & Interfaces 2015 v.7 no.9 pp. 5420-5428
acetylation, amines, cell viability, hemolysis, image analysis, iron oxides, mice, nanoparticles, neoplasms, receptors
This article reports a new approach for the synthesis of ultrasmall iron oxide nanoparticles (NPs) conjugated with Arg-Gly-Asp (RGD)-modified dendrimers (G5.NHAc-RGD-Fe₃O₄ NPs) as a platform for targeted magnetic resonance (MR) imaging of C6 glioma cells. Ultrasmall Fe₃O₄ NPs synthesized via a solvothermal route were conjugated with RGD peptide-modified generation-5 poly(amidoamine) dendrimers (G5.NH₂-RGD). The final G5.NHAc-RGD-Fe₃O₄ NPs were formed following the acetylation of the remaining dendrimer terminal amines. The as-prepared multifunctional Fe₃O₄ NPs were characterized using various techniques. The results of a cell viability assay, cell morphological observation, and hemolysis assay indicated that the G5.NHAc-RGD-Fe₃O₄ NPs exhibit excellent cytocompatibility and hemocompatibility over the studied concentration range. In addition, RGD conjugated onto the Fe₃O₄ NPs allows for the efficient targeting of the particles to C6 cells that overexpress αᵥβ₃ receptors, which was confirmed via in vitro cell MR imaging and cellular uptake. Finally, the G5.NHAc-RGD-Fe₃O₄ NPs were used in the targeted MR imaging of C6 glioma cells in mice. The results obtained from the current study indicate that the developed G5.NHAc-RGD-Fe₃O₄ NPs offer significant potential for use as contrast agents in the targeted MR imaging of different types of tumors.