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Preparation method of radiotherapy sensitization type hypoxia bimodal contrast agent based on dendritic macromolecules

A technology of dendrimers and reducing agents, applied in the preparation of X-ray contrast agents, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc.

Active Publication Date: 2019-05-24
DONGHUA UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0005] Searching the literature at home and abroad has not found any research on the use of functional dendrimer hybrid nanomaterials for hypoxia targeted imaging and radiosensitization of hypoxic tumors

Method used

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  • Preparation method of radiotherapy sensitization type hypoxia bimodal contrast agent based on dendritic macromolecules
  • Preparation method of radiotherapy sensitization type hypoxia bimodal contrast agent based on dendritic macromolecules
  • Preparation method of radiotherapy sensitization type hypoxia bimodal contrast agent based on dendritic macromolecules

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Experimental program
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Embodiment 1

[0068] (1) Dissolve 2-(2-nitroimidazol-1-yl)acetic acid (5.13mg) in 5mL DMSO, add 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide salt Acetate (11.5 mg) was activated for 30 min; then the above solution was added dropwise to 10 mL of polyethylene glycol (COOH-PEG-NH 2 , 40 mg) in DMSO solution, stirred at room temperature for 72 hours, and then used a dialysis bag with a molecular weight cut-off of 1000 to dialyze the aqueous solution for 3 days (2L / time, 3 times / day), and finally freeze-dried to obtain nitroimidazole-modified polyethylene glycol Ni-PEG-COOH;

[0069] (2) The fifth generation polyamide-amine dendrimer G5.NH 2 (20mg) was dissolved in 4mL of ultrapure water, added dropwise into an ultrapure aqueous solution of metal chelating agent DOTA active ester (DOTA-NHS, 11.71mg), stirred at room temperature for 24 hours, and then used a dialysis bag with a molecular weight cut-off of 5000 for the aqueous solution Dialyze for 3 days (2L / time, 3 times / day), and finally free...

Embodiment 2

[0071] The preparation method of G5.NHAc-DOTA is: take the G5.NH prepared in Example 1 (2) 2 -DOTA (20 mg) was dissolved in ultrapure water, added triethylamine (8.5 μL) and mixed evenly, then added dropwise acetic anhydride solution (6.9 μL), stirred at room temperature for 24 hours, and dialyzed the aqueous solution using a dialysis bag with a molecular weight cut-off of 5000 For 3 days (2 L / time, 3 times / day), freeze-dry to obtain G5.NHAc-DOTA.

[0072] The preparation method of G5.NHAc is: take the middle G5.NH 2 (20 mg) was dissolved in ultrapure water, and triethylamine (10.6 μL) was added to mix well, then acetic anhydride solution (8.7 μL) was added dropwise, stirred at room temperature for 24 hours, and the aqueous solution was dialyzed for 3 days using a dialysis bag with a molecular weight cut-off of 5000 (2L / time, 3 times / day), freeze-dried to obtain G5.NHAc.

Embodiment 3

[0074] With the G5.NH prepared in embodiment 1 (2) 2 - DOTA (20mg) was dissolved in water, 0.83mL HAuCl was added 4 4H 2 O aqueous solution (30mg / mL), stirred for 0.5h, then NaBH was added rapidly to it 4 (11.5 mg, 5 mg / mL) as a reducing agent, stirred overnight, and then dialyzed the aqueous solution for 3 days (2 L / time, 3 times / day) using a dialysis bag with a molecular weight cut-off of 8000-14000, and finally freeze-dried to obtain a hybrid Gold nanoparticles (Au 0 ) 100 -G5.NH 2 -DOTA;

[0075] Ni-PEG-COOH (26.19mg) in Example 1(1) was dissolved in ultrapure water, and then the aqueous solution dissolved in EDC (11.66mg) and NHS (8.4mg) was added dropwise for activation for 3 hours. The activated solution was added dropwise to the dissolved (Au 0 ) 100 -G5.NH 2 -In the aqueous solution of DOTA, after 3 days of magnetic stirring reaction, the aqueous solution was dialyzed for 3 days (2L / time, 3 times / day) using a dialysis bag with a molecular weight cut-off of 80...

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Abstract

The invention relates to a preparation method of a radiotherapy sensitization type hypoxia bimodal contrast agent based on dendritic macromolecules. The method includes directly complexing trivalent gold ions with functionalized dendritic macromolecules G5.NH2-DOTA and reducing to form hybrid gold nanoparticles (Au0)100-G5.NH2-DOTA; and modifying nitroimidazole-modified polyethyleneglycol on the hybrid gold nanoparticles through amide bonds to obtain functionalized gold nanoparticles (Au0)100-G5.NH2-DOTA-PEG-Ni, and then chelating and acetylating gadolinium ions to obtain a functionalized hybrid nano material Gd-Au DENPs-Ni. The material has good imaging performance and stability, and the prepared nano material achieves a radiotherapy sensitization effect by combining radiotherapy and hasa good application prospect.

Description

technical field [0001] The invention belongs to the field of preparation of functional hybrid nanomaterials, in particular to a preparation method of a dendrimer-based radiotherapy-sensitizing hypoxic dual-mode contrast agent. Background technique [0002] Radiotherapy is a local treatment method for tumors treated with radiation, and has become one of the most commonly used and effective methods for treating malignant tumors in clinical practice. However, in the course of clinical treatment, most tumors have a certain degree of radioresistance to radiotherapy. Studies have shown that in solid tumors, the proliferation of tumor cells and the incomplete development and uneven distribution of blood vessels lead to insufficient supply of oxygen, etc., which eventually leads to the existence of hypoxic areas in the tumor. The ability of tumor cells in this area to resist ionizing radiation exceeds 2 to 3 times that of normoxic tumor cells. Hypoxic regions of solid tumors reduc...

Claims

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Application Information

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IPC IPC(8): A61K41/00A61K47/10A61K49/04A61K49/12A61P35/00
Inventor 史向阳涂文志范钰刘勇
Owner DONGHUA UNIV
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