Method for preparing gadolinium-containing nano particles

A nanoparticle and gadolinium salt technology is applied in the field of preparation of gadolinium-containing nanoparticles to achieve the effects of improving relaxation efficiency and contrast effect.

Inactive Publication Date: 2010-06-30
TIANJIN UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Starting from changing the targeting mechanism of the liver contrast agent and reducing the dose, the receptor-mediated design is used to introduce small molecular substances with high liver targeting, such as glycyrrhetinic acid, cholic acid and folic acid, which are degradable and have good properties. On a biocompatible polymer carrier (such as chitosan, polyamino acid, etc.), the preparation of magnetic nanoparticles containing Gd through the electrostatic interaction of polydielectrics has not been reported in the literature

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Embodiment 1 Preparation of chitosan containing glycyrrhetinic acid group:

[0039] 1.1 Synthesis of carboxy-modified glycyrrhetinic acid derivatives:

[0040] Dissolve 4.70g of glycyrrhetinic acid in 30ml of N,N-dimethyl sulfoxide, cool, add 1.26g of diisopropylcarbodiimide, stir and add 1.15g of N-hydroxysuccinimide, at room temperature Stir the reaction, pour the reaction mixture into 100ml of absolute ethanol, collect the white solid, wash with 20ml of absolute ethanol, then wash with 10ml of absolute ether, and dry in vacuo to obtain the active ester of glycyrrhetinic acid;

[0041] Add the N,N-dimethylsulfoxide solution of glycyrrhetinic acid active ester dropwise to 200ml N,N-dimethylsulfoxide solution containing 28g of butanediamine, and react at 70°C for 15h, and the reaction solution Pour into 1000ml of water and place at 3°C. The precipitate was filtered, washed with 20 ml of ethanol and 100 ml of ether, dried, and the resulting precipitate was dissolved in...

Embodiment 2

[0045] Embodiment 2 Preparation of chitosan containing cholic acid groups:

[0046] 2.1 Synthesis of carboxy-modified cholic acid derivatives:

[0047] Dissolve 4.08g of cholic acid in 30ml of N,N-dimethylsulfoxide, cool, add 1.51g of diisopropylcarbodiimide, stir and add 1.38g of N-hydroxysuccinimide, and stir at room temperature For the reaction, the reaction mixture was poured into 140ml of absolute ethanol, and the white solid was collected, washed with 30ml of absolute ethanol, then washed with 20ml of anhydrous ether, and dried in vacuo to obtain the active ester of cholic acid;

[0048] Add the N,N-dimethylsulfoxide solution of bile acid active ester dropwise to 200ml N,N-dimethylsulfoxide solution containing 30g of butanediamine, and react at 70°C for 15h, and the reaction solution Pour into 1000ml of water and place at 3°C. The precipitate was filtered, washed with 25 ml of ethanol and 100 ml of ether, dried, and the obtained precipitate was dissolved in N,N-dimethy...

Embodiment 3

[0052] Example 3 Preparation of polylysine containing folic acid groups:

[0053] 3.1 Synthesis of carboxy-modified folic acid derivatives:

[0054] Dissolve 4.41g of folic acid in 30ml of N,N-dimethyl sulfoxide, cool, add 1.62g of diisopropylcarbodiimide, stir and add 1.42g of N-hydroxysuccinimide, and stir the reaction at room temperature , the reaction mixture was poured into 140ml of absolute ethanol, the white solid was collected, washed with 30ml of absolute ethanol, then washed with 20ml of anhydrous ether, and vacuum-dried to obtain the active ester of folic acid;

[0055] Add the N,N-dimethylsulfoxide solution of folic acid active ester dropwise to 200ml N,N-dimethylsulfoxide solution containing 34g butanediamine, react at 70°C for 15h, pour the reaction solution Pour into 1000ml of water and place at 3°C. The precipitate was filtered, washed with 25 ml of ethanol and 100 ml of ether, dried, and the obtained precipitate was dissolved in N,N-dimethylformamide, precip...

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Abstract

The invention relates to a method for preparing gadolinium-containing nano particles, belonging to the field of biomedicines. Liver-targeting compound and amido polymer are used to prepare polymer containing a liver-targeting group, which has ion crosslinking reaction with gadolinium brine solution to prepare the gadolinium-containing nano particles. The gadolinium-containing nano particles are used for MRI magnetic resonance imaging, and can evidently increase relaxivity and improve the imaging effect.

Description

technical field [0001] The invention belongs to the field of biomedicine, in particular to a method for preparing gadolinium-containing nanoparticles. Background technique [0002] According to the 2004-2010 "China Cancer Prevention and Control Program Outline", 8 cancer deaths including lung cancer, liver cancer, and gastric cancer accounted for more than 80% of the total cancer deaths in China. my country is an area with a high incidence of liver cancer, the incidence of primary liver cancer accounts for 45% of the world, the mortality rate ranks second in malignant tumors, and the 5-year survival rate is only 5%. The total course of liver cancer is about 2 and a half years, of which 2 years are in the early stage without symptoms. Once symptoms appear, most patients only have half a year to survive. If the small lesions can be detected in time in the early stage and surgically removed in time, the 5-year survival rate can reach 60%-70%. In imaging diagnosis of the liver...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K49/18A61K49/10A61K49/12
Inventor 查瑞涛张旖倩王立军
Owner TIANJIN UNIV OF SCI & TECH
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