The probable nanotoxicity to human health and the environment is a significant challenge for the sustainable application of nanomaterials in medicine. The cytototoxical effect of succimer (meso-2,3-dimercaptosuccinic acid-DMSA) coated titanium dioxide (DMSA-TiO
2
) with cultured human aortic endothelial cells (HAoECs) was assessed in this investigation. Our findings have shown that DMSA-TiO
2
can be accumulated in HAoECs and dispersed in a cytoplasm on the culture medium. DMSA-cytotoxicity TiO
2
effects were dose-responsive, and the concentrations were of little toxicity, and MTT stain testing showed that they had only 0.02 mg ml
−1
. Meanwhile, the lactate dehydrogenase biomarker was not considerably more remarkable than the biomarker from untreated (control) cells (free DMSA-TiO
2
). Though, also without any apparent signs of cell damage, the endocrine functions for prostacyclin I-2 and endothelin-1 and the urea transporter functions were modified. In addition,
in vitro
endothelial tube development has been shown that HAoECs could induce angiogenesis even with small amounts of DMSA-TiO
2
(0.01 and 0.02 mg ml
−1
). Further, we have examined the
in vivo
toxicity and biochemical parameter by animal model. Furthermore,
in vivo
assessments designated that the resulting DMSA-TiO
2
presented synergistic activities of angiogenesis activity. Overall, these findings show the cytotoxicity of DMSA-TiO
2
and could induce adverse effects on normal endothelial cells.