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EGFR receptor-targeted tumor diagnosis and treatment radioactive nanoparticles and preparation method thereof

A nanoparticle and radioactive technology, applied in the field of novel nanoparticles and their preparation, can solve problems such as the inability to achieve combined therapy

Inactive Publication Date: 2020-07-07
SHANGHAI ATOM KEXING PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, combined treatment of tumor radiotherapy-chemotherapy guided by PET / MRI / PAI fusion technology cannot be achieved

Method used

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  • EGFR receptor-targeted tumor diagnosis and treatment radioactive nanoparticles and preparation method thereof
  • EGFR receptor-targeted tumor diagnosis and treatment radioactive nanoparticles and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0067] The preparation method of radioactive nanoparticles for tumor diagnosis and treatment targeting tumor EGFR receptors of the present invention:

[0068] Take 8mmol PAA and 4mmol FeCl 3 Dissolve in diethylene glycol DEG (30mL), then transfer the above mixture into a 50mL three-necked flask, and place it in a microwave oven with vigorous stirring. When the temperature reached 220° C., 2 mL of NaOH solution (100 mg / mL, 80° C.) prepared in DEG was quickly added thereto. Further heating and mixing with a microwave heating power of 800W for 10 min, and cooling to room temperature of 20° C. to obtain a black colloid of iron oxide. The final product was obtained after centrifugation and washing.

[0069] Take 16.9mg AgNO 3 Dissolve in 1mL water, 15mg cisplatin is dissolved in 1mL water, AgNO 3 The solution was added dropwise to cisplatin, heated at 50°C for 1 h, and then centrifuged at 6000 r / min for 5 min to separate AgCl.

[0070] Take 1.5 mg of iron oxide nanoparticle su...

Embodiment 2

[0076] A tumor EGFR receptor-targeted radioactive nanoparticle is prepared by the following method:

[0077] (1) carrier preparation

[0078] Use ferric chloride, polyacrylic acid (PAA) and diethylene glycol (DEG), quickly add NaOH solution dissolved in DEG at 180 ° C, react for 15 minutes, and prepare iron oxide nanoparticles after cooling, in which ferric chloride and PAA The molar ratio of ferric chloride is 1:1, and the mass volume ratio of ferric chloride and DEG is 1:45mol / L;

[0079] (2) Cisplatin loading

[0080] The loading method of cisplatin is as follows: silver nitrate and cisplatin are mixed at a molar ratio of 1:1, react at 40°C to obtain cisplatin hydrate, then add cisplatin hydrate to the iron oxide nanoparticles prepared above for reaction, cisplatin hydrate Platinum and iron oxide nanoparticles were mixed at a mass ratio of 3:3, and stirred and reacted for 2 hours by magnetic stirring to obtain cisplatin-supported iron oxide nanoparticles;

[0081] (3) Do...

Embodiment 3

[0090] A tumor EGFR receptor-targeted radioactive nanoparticle is prepared by the following method:

[0091] (1) carrier preparation

[0092] Use ferric chloride, polyacrylic acid (PAA) and diethylene glycol (DEG), quickly add NaOH solution dissolved in DEG at 240 ° C, react for 5 minutes, and prepare iron oxide nanoparticles after cooling, in which ferric chloride and PAA The molar ratio of ferric chloride is 1:3, and the mass volume ratio of ferric chloride and DEG is 1:55mol / L;

[0093] (2) Cisplatin loading

[0094] The loading method of cisplatin is as follows: silver nitrate and cisplatin are mixed at a molar ratio of 5:1, react at 60°C to obtain cisplatin hydrate, then add cisplatin hydrate to the iron oxide nanoparticles prepared above for reaction, cisplatin hydrate Platinum and iron oxide nanoparticles were mixed at a mass ratio of 3:6, and stirred and reacted by magnetic stirring for 0.5h to obtain cisplatin-supported iron oxide nanoparticles;

[0095] (3) Dopami...

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Abstract

The invention relates to EGFR receptor-targeted radioactive nanoparticles and a preparation method thereof. The nanoparticles consist of iron oxide nanoparticles with a particle size of 5-10 nm, polyacrylic acid, cis-platinum, dopamine, GE11 small peptides (Y-H-W-Y-G-Y-T-P-Q-N-V-I-K-(CH2)m-N3) containing tyrosine, histidine, tryptophan, tyrosine, glycine, tyrosine, threonine, proline, glutamine, asparagine, valine, isoleucine, lysine and azidoacetic acid, and radionuclide containing copper-64 (64Cu). Compared with the prior art, the nanoparticles prepared by the method can be used for radiotherapy-chemotherapy combined treatment guided by PET / MRI / PAI imaging diagnosis.

Description

technical field [0001] The invention relates to a novel nanoparticle and a preparation method thereof, in particular to a tumor EGFR receptor-targeted, cisplatin-loaded, radionuclide-labeled nanoparticle and a preparation method thereof. Background technique [0002] The morbidity and mortality of tumors are increasing year by year, and people have been actively exploring how to achieve a radical cure for tumors. Single treatment methods such as chemotherapy, radiotherapy, photothermal therapy, immunotherapy and other treatment methods have their limitations, so the treatment effect is still not ideal. With the development of nanotechnology, the integration of multiple therapeutic strategies into a single nanocarrier-based platform has proven to be effective. [0003] However, the combination of radiotherapy and chemotherapy is still the most commonly used strategy for cancer treatment. Chemotherapy is the treatment of cancer cells by using chemotherapy drugs to kill cance...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/51A61K33/243A61K47/69A61K47/18A61K47/60A61K47/64A61K51/04A61K51/12A61P35/00
CPCA61K9/5123A61K33/24A61K51/0406A61K51/1251A61K47/60A61K47/64A61K47/6923A61P35/00
Inventor 曹本红
Owner SHANGHAI ATOM KEXING PHARMA
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