The invention provides a specific targeting radionuclide marker and a preparation method and application thereof, belonging to the technical field of nanomedicine and molecular imaging. The present invention uses graphene-based tumor cell nucleus targeting fluorescent nanoprobes (GTTN) as a nucleus targeting molecule to label radionuclides, and the obtained markers can be directly used for single photon emission computed tomography (SPECT) and positrons in the tumor area Transmitting computed tomography (PET), and radionuclide therapy can be performed; in addition, the marker can not only use GTTN's cell membrane permeability targeting mechanism to highly target the tumor area, but also can pass GTTN's fluorescence imaging and radioactivity Radionuclide SPECT or PET imaging can achieve dual-modality imaging to achieve precise diagnosis and treatment effects, while minimizing the side effects of radionuclides on normal tissues, which has a good clinical application prospect.
The role and status of radiotherapy in tumor treatment have become increasingly prominent, and it has become one of the main methods for the treatment of malignant tumors. Radionuclides used for radiotherapy can not only be used as radiopharmaceuticals in tumor treatment, but also as radioactive probes for tumor imaging. However, radiotherapy still has many shortcomings, such as rapid excretion of radionuclides after intravenous injection, non-specific systemic distribution, and relatively low tumor uptake. In addition, low-dose radionuclides have a certain lethality to tumors, but may make cancer cells resistant to radiotherapy, while high-dose radionuclides can destroy normal cells and cause serious side effects, such as dysfunction and Disorders, lack of energy, decreased appetite, physical weakness, fatigue, nausea and vomiting, fullness after eating, etc., and can cause skin and mucous membrane diseases. These serious side effects restrict the dose and effect of radiotherapy. In order to achieve the best tumor treatment effect while minimizing side effects on normal tissues, there is an urgent need to develop a tumor-targeted radionuclide delivery platform.
The purpose of the present invention is to provide a specific targeting radionuclide marker and its preparation method and application. The present invention uses graphene-based tumor cell nucleus targeting fluorescent nanoprobe as the nucleus targeting molecule to label the radionuclide. Specific targeting radionuclide markers can achieve dual-modal imaging, achieve precise diagnosis and treatment effects, and have good clinical application prospects.
The present invention provides a specific targeting radionuclide marker, including a graphene-based tumor cell nucleus targeting fluorescent nanoprobe, a connection reagent, and a radionuclide. The graphene-based tumor cell nucleus targeting fluorescent nanoprobe The needle, the connecting reagent and the radionuclide are sequentially covalently connected; wherein the graphene-based tumor cell nuclear targeting fluorescent nanoprobe and the connecting reagent are connected by an amide bond.
Patent number:CN202010278513.4
