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首页> 外文期刊>Theranostics >Tumor-penetrating Peptide Conjugated and Doxorubicin Loaded T1-T2 Dual Mode MRI Contrast Agents Nanoparticles for Tumor Theranostics
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Tumor-penetrating Peptide Conjugated and Doxorubicin Loaded T1-T2 Dual Mode MRI Contrast Agents Nanoparticles for Tumor Theranostics

机译：肿瘤穿透肽共轭和阿霉素负载的T 1 -T 2 双模式MRI造影剂纳米颗粒用于肿瘤治疗

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The conventional chemotherapeutics could not be traced in vivo and provide timely feedback on the clinical effectiveness of drugs. Methods: In this study, a tumor-penetrating peptide RGERPPR (RGE) modified, Gd-DTPA conjugated, and doxorubicin (DOX) loaded Fe3O4@SiO2@mSiO2 nanoparticle drug delivery system (Fe3O4@SiO2@mSiO2/DOX-(Gd-DTPA)-PEG-RGE NPs) was prepared for tumor theranostics. Results: The Fe3O4@SiO2@mSiO2/DOX-(Gd-DTPA)-PEG-RGE NPs showed a z-average hydrodynamic diameter of about 90 nm, and a pH-sensitive DOX release profile. The 3 T MRI results confirmed the relaxivity of the NPs (r1 = 6.13 mM-1S-1, r2 = 36.89 mM-1S-1). The in vitro cellular uptake and cytotoxicity assays on U87MG cells confirmed that the conjugation of RGERPPR played a significant role in increasing the cellular uptake and cytotoxicity of the NPs. The near-infrared fluorescence in vivo imaging results showed that the NPs could be significantly accumulated in the U87MG tumor tissue, which should result from the mediation of the tumor-penetrating peptide RGERPPR. The MRI results showed that the NPs offered a T1-T2 dual mode contrast imaging effect which would lead to a more precise diagnosis. Compared with unmodified NPs, the RGE-modified NPs showed significantly enhanced MR imaging signal in tumor tissue and antitumor effect, which should also be attributed to the tumor penetrating ability of RGERPPR peptide. Furthermore, the Hematoxylin and Eosin (H&E) staining and TUNEL assay proved that the NPs produced obvious cell apoptosis in tumor tissue. Conclusions: These results indicated that Fe3O4@SiO2@mSiO2/DOX-(Gd-DTPA)-PEG-RGE NPs are an effective targeted delivery system for tumor theranostics, and should have a potential value in the personalized treatment of tumor.
机译：无法在体内追踪到常规化学疗法，无法及时提供有关药物临床疗效的反馈。方法：在这项研究中，肿瘤穿透肽RGERPPR（RGE）修饰，Gd-DTPA共轭和阿霉素（DOX）负载Fe 3 O 4 @SiO 2 @mSiO 2 纳米颗粒药物递送系统（Fe 3 O 4 @SiO 2 @制备了mSiO 2 / DOX-（Gd-DTPA）-PEG-RGE NPs用于肿瘤治疗。结果：Fe 3 O 4 @SiO 2 @mSiO 2 / DOX-（Gd-DTPA）- PEG-RGE NPs的z平均流体动力学直径约为90 nm，并且具有pH敏感的DOX释放曲线。 3 T MRI结果证实了NPs的弛豫性（r 1 = 6.13 mM -1 S -1 ，r 2 < / sub> = 36.89 mM -1 S -1 ）。在U87MG细胞上进行的体外细胞摄取和细胞毒性测定证实，RGERPPR的缀合在增加NP的细胞摄取和细胞毒性方面起着重要作用。近红外荧光体内成像结果表明，NPs可能在U87MG肿瘤组织中大量积累，这应该是由穿透肿瘤的肽RGERPPR介导的。 MRI检查结果表明，NPs具有T 1 -T 2 双模对比成像的作用，有助于诊断的准确性。与未修饰的NP相比，RGE修饰的NP在肿瘤组织中显示出显着增强的MR成像信号和抗肿瘤作用，这也应归因于RGERPPR肽的肿瘤穿透能力。此外，苏木精和曙红（H＆E）染色和TUNEL分析证明，NPs在肿瘤组织中产生明显的细胞凋亡。结论：这些结果表明Fe 3 O 4 @SiO 2 @mSiO 2 / DOX-（Gd- DTPA）-PEG-RGE NPs是一种有效的肿瘤治疗学靶向递送系统，在肿瘤的个性化治疗中应具有潜在价值。

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