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Updated: Jul 16, 2025
A Comprehensive Procedure to Evaluate the In Vivo Performance of Cancer Nanomedicines
Published on: March 4, 2017
Multimodal Imaging-Guided Strategy for Developing 177Lu-Labeled Metal-Organic Framework Nanomedicine with Potential
Ranxi Liang1,2, Feize Li1, Xijian Chen1
1Key Laboratory of Radiation Physics and Technology of the Ministry of Education, Institute of Nuclear Science and Technology, Sichuan University, Chengdu 610064, P. R. China.
Abstract:
Nano-metal-organic frameworks (nano-MOFs) labeled with radionuclides have shown great potential in the anticancer field. In this work, we proposed to combine fluorescence imaging (FI) with nuclear imaging to systematically evaluate the tumor inhibition of new nanomedicines from living cancer cells to the whole body, guiding the design and application of a high-performance anticancer radiopharmaceutical to glioma. An Fe-based nano-MOF vector, MIL-101(Fe)/PEG-FA, was decorated with fluorescent sulfo-cyanine7 (Cy7) to investigate the binding affinity of the targeting nanocarriers toward glioma cells in vitro, as well as possible administration modes for in vivo cancer therapy. Then, lutetium-177 (177Lu)-labeled MIL-101(Fe)/PEG-FA was prepared for high-sensitive imaging and targeted radiotherapy of glioma in vivo. It has been demonstrated that the obtained 177Lu-labeled MIL-101(Fe)/PEG-FA can work as a complementary probe to rectify the cancer binding affinity of the prepared nanocarrier given by fluorescence imaging, providing more precise biodistribution information. Besides, 177Lu-labeled MIL-101(Fe)/PEG-FA has excellent antitumor effect, leading to cell proliferation inhibition, upregulation of intracellular reactive oxygen species, tumor growth suppression, and immune response-related protein and cytokine upregulation. This work reveals that optical imaging and nuclear imaging can work complementarily as multimodal imaging in the design and evaluation of anticancer nanomedicine, offering a MIL-101(Fe)/PEG-FA-based pharmaceutical with potential in tumor endoradiotherapy.
Insights
This study combines fluorescence and nuclear imaging to evaluate a novel iron-based nano-metal-organic framework (nano-MOF) for targeted glioma therapy. The radiolabeled nano-MOF shows promise for precise cancer imaging and effective endoradiotherapy.
Area of Science:
- Biomedical Engineering
- Radiopharmaceutical Chemistry
- Nanomedicine
Background:
- Nano-metal-organic frameworks (nano-MOFs) are emerging as promising agents in anticancer therapy.
- Combining fluorescence imaging (FI) and nuclear imaging offers enhanced capabilities for evaluating nanomedicines.
Purpose of the Study:
- To develop and evaluate a novel Fe-based nano-MOF, MIL-101(Fe)/PEG-FA, for multimodal imaging and targeted glioma therapy.
- To investigate the complementary roles of FI and nuclear imaging in assessing nanomedicine efficacy.
- To guide the design of high-performance anticancer radiopharmaceuticals for glioma.
Main Methods:
- Decoration of MIL-101(Fe) with PEG-FA and fluorescent sulfo-cyanine7 (Cy7) for in vitro binding affinity studies.
- Preparation of lutetium-177 (177Lu)-labeled MIL-101(Fe)/PEG-FA for in vivo imaging and radiotherapy.
- Systematic evaluation of tumor inhibition using combined fluorescence and nuclear imaging techniques.
Main Results:
- Fluorescence imaging confirmed nanocarrier binding affinity to glioma cells in vitro.
- 177Lu-labeled MIL-101(Fe)/PEG-FA provided precise biodistribution information, complementing FI data.
- The radiolabeled nano-MOF demonstrated significant antitumor effects, including cell proliferation inhibition, increased reactive oxygen species, tumor growth suppression, and immune response modulation.
Conclusions:
- Multimodal imaging using optical and nuclear techniques is effective for evaluating anticancer nanomedicines.
- MIL-101(Fe)/PEG-FA, labeled with 177Lu, shows potential as a radiopharmaceutical for glioma endoradiotherapy.
- This approach aids in the design and application of advanced nanomedicines for cancer treatment.
