Metal nano-cluster containing radioactive metal nuclide, nano-material, preparation method of metal nano-cluster containing radioactive metal nuclide, preparation method of nano-material containing radioactive metal nuclide

A technology of metal nanoclusters and nanomaterials, applied in the field of metal nanoclusters, can solve the problems of simultaneous labeling of multiple nuclides, damage to tissues and organs, and large particle size, so as to achieve broad-spectrum labeling, improve stability, and enhance stability sexual effect

Pending Publication Date: 2022-02-22
SHANGHAI JIAO TONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] 1. Most of the existing nuclide labeling methods use chelating agents such as DOTA to couple the nuclide to the drug carrier. The introduction of the chelating agent will affect the pharmacokinetic behavior of the drug, and the nuclide is easy to fall off, causing damage to normal tissues or organs. greater harm;
[0006] 2. The existing method of internal labeling of nuclides can only label a few nuclides with similar chemical properties to the carrier elements, which limits the simultaneous labeling of multiple nuclides;
[0007] 3. The existing labeling methods of nuclear medicine are required to be carried out in a smaller reaction system to improve the labeling efficiency. The reaction volume is tens to hundreds of microliters. Although the reaction in a small system can improve the labeling efficiency, it limits the radiopharmaceuticals. Large-scale synthesis and preparation of
[0008] 4. Most of the radioactive nano-pharmaceuticals reported so far have the problems of large particle size, poor behavior in the body, and a large amount of accumulation in the liver and spleen, causing great damage to normal tissues and organs

Method used

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  • Metal nano-cluster containing radioactive metal nuclide, nano-material, preparation method of metal nano-cluster containing radioactive metal nuclide, preparation method of nano-material containing radioactive metal nuclide
  • Metal nano-cluster containing radioactive metal nuclide, nano-material, preparation method of metal nano-cluster containing radioactive metal nuclide, preparation method of nano-material containing radioactive metal nuclide
  • Metal nano-cluster containing radioactive metal nuclide, nano-material, preparation method of metal nano-cluster containing radioactive metal nuclide, preparation method of nano-material containing radioactive metal nuclide

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0077] In this example, a GS is coated with a C (RGDYC) cyclic small peptide. 177 Luau NCS (referred to as RGD-GS- 177 A Case Study of Radioactive Nano Materials and Synthesis Methods. RGD-GS- 177 LUAU NCS, HAUCL 4 Reduced by GSH and cyclic RGD small peptide C (RGDYC) into gold nanoclusters, 177 The LU is doped into the lattice of the gold nanocluster in the form of atoms, and the final product is a colorless transparent liquid. The final product of purification is GS-containing cyclic small peptide C (RGDYC). 177 LUAU NCS. The final reaction pH of the present embodiment is about 7.0, and the reaction temperature is 60 ° C.

[0078] The preparation method includes the steps of:

[0079] (1), add 5 ml of ultra-pure water in the reaction bottle, then add 40 μl of concentration of 250 mm to Haucl 4 · 3h 2 O and 3MCI 177 LUCL 3 (3 μL), mixed mixed with stirring and mixed with reduced glutathione (RGDECED GSH) with a concentration of 100 mm from 100 μl of concentration of 1 mg / ml, an...

Embodiment 2

[0091] In this example, a GS-coated RGD cycloin peptide. 68 GAAU NCS (referred to as RGD-GS- 68 Take the radioactive nanomaterial and its synthesis method.

[0092] RGD-GS- 68 Gaau NCS, Haucl 4 Restored by GSH and RGD cyclonic C (RGDYC) into gold nanoclusters, 68 GA is doped into the lattice of the gold nanocluster in the form of atoms. The final product is a colorless transparent nanoparticle suspension. The final reaction pH of the present embodiment is 6.8, and the reaction temperature is 50 ° C.

[0093] The preparation method includes the steps of:

[0094] (1), add 5 ml of ultra-pure water in the reaction bottle, then add 40 μl of concentration of 250 mm to Haucl 4 · 3h 2 O and 3MCI 68 GaCl 3 (100 μL, 0.05 M HCl), mixed mixed with stirring, adding 5 μl of concentration of 1.0 M in the mixture to neutralize 68 GaCl 3 The introduced hydrochloric acid solution. Then, 200 μl of a reduced glutathione (RGD GSH) having a concentration of 1 mg / ml was added dropwise to a mixed syst...

Embodiment 3

[0101] In this example, a GS is coated with a C (RGDYC) cyclic small peptide. 68 GA 177 Luauncs (referred to as RGD-GS- 68 GA 177 A Case Study of Radioactive Nano Materials and Synthesis Methods.

[0102] RGD- 68 GA 177 LUAUNCS, HAUCL 4 Restored by GSH and RGD Total peptide C (RGDYC) into gold nanoclusters, 68 GA and 177 The LU is doped into the lattice of the gold nanoclassical in the form of atom. The final product is a colorless transparent nanoparticle suspension. The final reaction pH of the present embodiment is 7.5, and the reaction temperature is 70 ° C.

[0103] The preparation method includes the steps of:

[0104] (1), add 5 ml of ultra-pure water in the reaction bottle, then add 40 μl of concentration of 250 mm to Haucl 4 · 3h 2 O, 3MCI 177 LUCL 3 (3μL) and 3MCI 68 GaCl 3 (100 μL, 0.05 M HCl), mixed mixed with stirring, NaOH of 5 μl of left and right concentrations of 1.0 M in the mixture, neutralized 68 GaCl 3 The introduced hydrochloric acid solution. Then, 200 μl of...

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Abstract

The invention relates to a metal nano-cluster containing radioactive metal nuclide, a nano-material, a preparation method of the nano-cluster and the nano-material and application of the nano-cluster and the nano-material in preparation of and the metal nano-cluster containing the radioactive metal nuclide is characterized in that the metal nano-cluster containing the radioactive metal nuclide comprises the radioactive metal nuclide and a metal nano-cluster; and the radioactive metal nuclide is doped in the metal nano-cluster. According to the metal nano-cluster containing the radioactive metal nuclide, the nano-material containing the radioactive metal nuclide, the preparation methods of the nano-cluster and the nano-material and the application of the nano-cluster and the nano-material in preparation of targeted drugs, nuclide labeling based on the metal nano-cluster and without chelating agent ligands is achieved, the influence of the chelating agent ligands on in-vivo behaviors of the nano-drugs is avoided, and the stability of nuclide labeling is enhanced. According to the invention, various radioactive metal nuclides are individually or simultaneously labeled, and the application of the radioactive metal nuclides in radioactive nano-drugs is broadened. According to the method, nuclides can still be efficiently labeled under the large-system condition, and large-batch synthesis of radioactive nano-drugs is promoted.

Description

Technical field [0001] The present invention relates to metal nanocuses, nanomaterials, and preparation methods thereof, and applications thereof in the preparation of target drugs. Background technique [0002] Radioactive nano drugs play an increasingly important role in the diagnosis and treatment of various diseases, and one of the key technologies to construct radioactive nano drugs is to achieve efficient and stable nucleoside markers. With the continuous development of nuclear medicine and nanotechnology, a variety of nanomaterials have been proposed. Methods that have now been reported are mainly divided into two categories: oral markers and nucleoside markers. Outer tags are currently the most commonly used method of radioactive drug tag, which combines a chelating agent with a nucleate, and then achieves rapid and efficient marking, and the commonly used chelating agent mainly has DOTA (1, 4, 7, 10- Tetrazo heterocyclic dodecane-1,4,7,10-tetracetic acid), NOTA (1,4,7-az...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K51/02A61K51/08A61P35/00A61K103/00A61K103/30A61K103/32
CPCA61K51/02A61K51/08A61P35/00A61K51/00A61K51/04
Inventor 张春富吴庆河
Owner SHANGHAI JIAO TONG UNIV
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