Nanomedicine can improve the traditional disease treatment by actively targeting and enhancing the controlled release of drugs in the focus tissue in vivo, moreover the integration of diagnosis and treatment can be achieved by using tracer molecules to indicate the accumulation of nanodrugs in the focus. However ， almost all chemotherapeutic drugs and gene drugs failed to effectively treat glioblastoma (GBM) on account of the existence of blood-brain barrier (BBB) which play a role in GBM. So far, the survival rate of patients with GBM has been hardly improved. In the present study, we constructed an integrated nanoprobe based on albumin nanoparticles (NPs) for targeted diagnosis and treatment of GBM. The nanoprobe consists of albumin-coated superparamagnetic iron oxide (SPIO), Carmustine (BCNU) and indocyanine green (ICG) to achieve bimodal imaging and drug delivery. And the surface-coupled Angopep-2 (ANG, TFFYGGSRGKRNNFKTEEY) polypeptide can specifically bind to low density lipoprotein receptor-related protein (LRP), which is overexpressed in BBB and GBM cells.
In the in vitro experiments, we verified that the targeting ability of nanoprobes to GBM cells was significantly better than that of the control group. In addition, in the in vivo experiments, nanoprobes significantly increased the accumulation of brain tumors compared with the control group. Cell killing of GBM cells (U87MG) with ANG-BSA/BCNU/ICG magnetic NPs shows a higher inhibitory effect compared with controls. This novel targeting imaging and drug delivery system provides an efficient strategy for targeted therapy and intraoperative localization of GBM.