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. 2021 Jan 1;11(2):579–601. doi: 10.7150/thno.48811

Table 1.

Summary of tumor-targeted, MRI-traceable nanotheranostics for drug-delivery applications

Targeting strategy In vivo tumor model Drug Purpose of investigation Important outcome(s) Ref
Integrin-targeting RGD and VEGFR-targeting GX1 peptide Hepatocellular carcinoma (HepG2) DOX Develop a dual integrin & VEGFR-targeted nanotheranostic platform Groups treated with dual-ligand probes demonstrated significantly higher tumor inhibition rate compared to groups treated with single ligand probes 46
pH-responsive H7K(R2)2 peptide Breast cancer (MDA-MB-231) PTX Develop an MRI-traceable, pH-responsive SPIONs Tumor size of mice treated with the targeted agent was significantly lower compared to mice treated with non-targeted SPIONs 41
Anti-PSMA peptide targeting PSMA Prostate cancer (LNCaP) Enzalutamide and BEZ235 Develop a theranostic agent for targeted dual drug delivery to castration-resistant prostate cancer Treatment with dual-drug carrying nanoparticles resulted in complete tumor regression of LNCaP tumor xenografts, in contrast to animals treated with a combination of both drugs in their free form 60
MT Colon cancer (CT-26) PTX Develop stimuli-responsive SIONR for controlled release of PTX Mice treated with PTX- pluronic F127- SIONR showed a higher therapeutic response and higher survival rate compared to mice treated with PTX alone 63
MT Glioma (U87MG) PTX Evaluate MT efficiency and antitumor efficacy of magnetically guided PTX/SPIO-NPs in an orthotopic glioblastoma tumor model MT resulted in the disruption of the BBB and enhanced accumulation of agent in the brain area of glioblastoma tumor-bearing mice; MT prolonged the median survival rate of glioblastoma tumor-bearing mice compared to PT and control groups 39
RGD targeting αvβ3 integrin & MT Glioma (U87MG) DOX Investigate targeting efficiency differences between PT, AT, MT, and dual AT+MT Tumors treated with RGD-DOX-MuMVs/magnet+ had the highest T2 contrast and highest antitumor efficacy 48
RGD targeting αvβ3 integrin & MT Cervical cancer (HeLa) DOX Develop a targeted theranostic nanoprobe for intracellular redox-sensitive drug release MT MMSN demonstrated the highest accumulation in the tumor, enhanced MRI contrast and highest therapeutic efficiency 49
T7 peptide targeting transferrin receptor & MT Glioma cancer (U87-Luc) PTX and CUR Develop dual AT+MT NP for codelivery of PTX and CUR to a brain tumor Combination treatment resulted in significantly enhanced treatment efficacy vs. individual treatment and vs. the combination of free drugs 61
Coating with the source cancer cell membranes Different types of tumors DOX Investigate the self- recognition of CCCM-coated DOX- conjugated Fe3O4 MNPs by homotypic cancer cells and homologous tumors Coating the surface of NPs with specific cell membranes obtained from different cancer cell lines led to the self- recognition internalization of NPs by the source cancer cells in vitro and homologous tumors in vivo 55
AS1411 aptamer targeting nucleolin Colon cancer (C26) DOX Develop anti-nucleolin-targeted magnetic PLGA nanoparticles as a theranostic agent Median survival time of mice treated with sucrose 10%, free Dox solution, NPs, and Apt-NPs were 21, 5, 34 and 42 days, respectively 69
MT Glioma (C6) CGT Develop theranostic liposome integrated with SPIONs, QDs, and CGT to target and inhibit integrin receptors MT resulted in enhanced delivery of agent into the tumor region, effective inhibition of tumors, and real-time image-guided accurate surgical resection of glioma tumors 77

Abbreviations: AT: Active targeting; BBB: blood-brain-barrier; CCCM: cracked cancer cell membranes; CGT: cilengitide; CUR: curcumin; MMSN: magnetic mesoporous silica nanoparticle; MT: magnetic targeting; MuMVs: multilayered magneto-vesicles; NP: nanoparticles; PT: passive targeting; PSMA: prostate-specific membrane antigen; PTX: paclitaxel; QDs: quantum dots; RGD: Arg-Gly-Asp; SIONRs: superparamagnetic iron oxide nanorods; SPION: superparamagnetic iron oxide nanoparticles; VEGFR: vascular endothelial growth factor receptor