A glutathione-activated co-assembled nanoprobe and its preparation method and application

By constructing the amphiphilic small molecule probes 1-Zn-PPA and 1-NLG, the limitations of existing tumor diagnosis and treatment probes in imaging and treatment are solved, and accurate tumor imaging and multi-mode treatment are achieved, effectively inhibiting tumor metastasis.

CN116173204BActive Publication Date: 2025-08-15NANJING UNIV +1
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Patent Information

Application Number
CN202211142252.9
Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
Filing Date
2022-09-20
Publication Date
2025-08-15
Estimated Expiration
2042-09-20

AI Technical Summary

Technical Problem

The existing tumor diagnosis and treatment probes have a single imaging mode in tumor imaging and treatment that is difficult to achieve accurate imaging. A single treatment method has limited ability to treat tumors, especially for recurrent and metastatic tumors.

Method used

The amphiphilic small molecule probes 1-Zn-PPA and 1-NLG were constructed, and co-assembled nanoprobes 1-NPs were formed, and the tumor site was aggregated by the tumor EPR effect and the targeting of the probe surface cRGD, and the hydrophilic small molecule containing Gd, the photo/acoustic drug Zn-PPA-SH and the immune adjuvant drug NLG919 were deassembled in the reduction environment of glutathione (GSH), to realize the combined treatment of acoustic dynamic therapy, photodynamic therapy and immunotherapy.

Benefits of technology

High-resolution and highly sensitive accurate imaging of tumors is achieved, and through the combination of sound-photodynamic therapy and immunotherapy, it effectively inhibits tumor metastasis, reduces the side effects of heavy metal toxicity, and enhances the therapeutic effect.

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Abstract

The present invention provides a glutathione-activated co-assembled nanoprobe and a preparation method and application thereof, belonging to the technical fields of chemical synthesis, biological analysis and detection, tumor imaging and treatment. In the present invention, amphiphilic small molecule probes 1-Zn-PPA and 1-NLG are constructed, and the probes 1-Zn-PPA and 1-NLG can be co-assembled in a solution to form co-assembled nanoprobes 1-NPs. The nanoprobes 1-NPs can accumulate at the tumor site under the tumor EPR effect and the targeting action of cRGD on the probe surface, and disassemble under the action of GSH present in the tumor reducing environment to release Gd-containing hydrophilic small molecule 2-Gd, light / sound-sensitive drug Zn-PPA-SH and immune adjuvant drug NLG919. The nanoprobes 1-NPs can realize combined sonodynamic therapy / photodynamic therapy / immunotherapy of living tumors. The nanoprobes 1-NPs have good applications in fluorescence imaging, magnetic resonance imaging, and the preparation of tumor treatment drugs and tumor-killing devices.
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