Tree polymer target contrast agent and preparation method thereof

A technology for targeting contrast agents and polymers, applied in the fields of biomedicine and nanomedicine, to achieve the effect of no immunogenicity and cytotoxicity, conducive to early detection and improved sensitivity

Inactive Publication Date: 2009-11-25
EAST CHINA NORMAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Folic acid residues are bonded to the surface of dendrimers through biocompatible macromolecules to synthesize particles with specific nanoscale sizes, and use

Method used

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  • Tree polymer target contrast agent and preparation method thereof
  • Tree polymer target contrast agent and preparation method thereof
  • Tree polymer target contrast agent and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] 1. Synthesis of PAMAM

[0035] a) Synthesis of 0.5G PAMAM-Me

[0036]Take 9g of ethylenediamine and 30g of methanol, and add 103.2g of methyl acrylate dropwise while stirring at a rate of one drop per second in a three-necked flask, and stir at 25°C for 24h. Then the product was distilled under reduced pressure at -5°C and 133.3Pa for 3 hours to obtain a pale yellow liquid.

[0037] b) 1.0G PAMAM-NH 2 Synthesis

[0038] Take 20.2g of 0.5 generation AMAM in a three-necked flask, add 60g of methanol, stir, add 72g of ethylenediamine dropwise at a rate of 1d / s, and stir at 25°C for 24h. Then the product was distilled under reduced pressure at -5°C and 266.6Pa for 3 hours to obtain a light yellow viscous liquid, namely 1.0G PAMAM-NH 2 .

[0039] c) Repeat steps a) and b) until pure 4.0G PAMAM is obtained

[0040] 2. Synthesis of PAMAM-COOH

[0041] Take 0.2mmol of PAMAM (4.0 generation) and dissolve in anhydrous DMSO, N 2 For protection, add 0.02mmol catalyst DMAP a...

Embodiment 2

[0049] 1. Synthesis of PAMAM

[0050] a) Synthesis of 0.5G PAMAM-Me

[0051] Take 9g of ethylenediamine and 30g of methanol, and add 103.2g of methyl acrylate dropwise while stirring at a rate of one drop per second in a three-necked flask, and stir at 25°C for 24h. Then the product was distilled under reduced pressure at -5°C and 133.3Pa for 3 hours to obtain a light yellow liquid, namely 0.5G PAMAM-Me.

[0052] b) 1.0G PAMAM-NH 2 Synthesis

[0053] Take 20.2g of 0.5 generation AMAM in a three-necked flask, add 60g of methanol, stir, add 72g of ethylenediamine dropwise at a rate of 1d / s, and stir at 25°C for 24h. Then the product was distilled under reduced pressure at -5°C and 266.6Pa for 3 hours to obtain a light yellow viscous liquid, namely 1.0G PAMAM-NH 2 .

[0054] c) Repeat steps a) and b) until pure 4.0G PAMAM is obtained

[0055] 2. NH 2 -PEG (2000) -Synthesis of FA

[0056] Dissolve 0.2mol of FA in DMSO, stir, N 2 For protection, add EDC / NHS to activate fo...

Embodiment 3

[0064] 1. Synthesis of PAMAM

[0065] a) Synthesis of 0.5G PAMAM-Me:

[0066] Take 9g of ethylenediamine and 30g of methanol, and add 103.2g of methyl acrylate dropwise while stirring at a rate of one drop per second in a three-necked flask, and stir at 25°C for 24h. Then the product was distilled under reduced pressure at -5°C and 133.3Pa for 3 hours to obtain a pale yellow liquid.

[0067] b) 1.0G PAMAM-NH 2 Synthesis

[0068] Take 20.2g of 0.5 generation AMAM in a three-necked flask, add 60g of methanol, stir, add 72g of ethylenediamine dropwise at a rate of 1d / s, and stir at 25°C for 24h. Then the product was distilled under reduced pressure at -5°C and 266.6Pa for 3 hours to obtain a light yellow viscous liquid, namely 1.0G PAMAM-NH 2 .

[0069] c) Repeat steps a) and b) until pure 4.0G PAMAM is obtained

[0070] 2. NH 2 -PEG (4000) -Synthesis of FA

[0071] Dissolve 0.2mol of FA in DMSO, stir, N 2 For protection, add EDC / NHS to activate for 2h, and then put in ...

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Abstract

The invention discloses a tree polymer target contrast agent and preparation method thereof, and the contrast agent is nanoparticle, which has the structure as follows: a target radical T is located on the outerest end; a hydrophilic polyethylene glycol chain is used as a connecting arm; a tree polymer PAMAM is located in the central nucleus; paramagnetic metal X is imaged in vivo; the general formula thereof is PAMAM-PEG[(n)]-T/X. The preparation method has the steps of: PEG with different molecular masses is reacted with the target radical for preparing a product with a target radical on one end and a amino on the other end: NH[2]-PEG[(n)]-T; NH[2]-PEG[(N)]-T is reacted with PAMAM-COOH with molar ratio 32:1 for preparing a macromolecular ligand; T-PEG[(N)]-PAMAM; The ligand is chelated with paramagnetic metallic ion solution for preparing PAMAM- PEG[(N)]-T/X. The preparation method provided by the invention has the advantages of simple operation, mild and safe condition and wide application. And the prepared contrast agent has small cell toxicity, high relaxivity, and very good imaging effect for white mouse in vivo; obvious target property for imaging of tumor - bearing nude mouse in vivo.

Description

technical field [0001] The invention belongs to the technical field of biomedicine and nanomedicine, and relates to a dendrimer targeting contrast agent and a preparation method thereof, in particular to a contrast agent for high-sensitivity MRI imaging of lung cancer. Background technique [0002] Cancer is becoming an increasingly serious global problem. At present, almost 7 million people die from cancer every year. The main types of cancer are: lung cancer (about 1.3 million deaths / year), gastric cancer (about 1 million deaths / year), liver cancer (about 66 10,000 deaths / year), colon cancer (approximately 66 deaths / year), and breast cancer (approximately 500,000 deaths / year), with lung cancer causing more deaths than any other cancer. Lung cancer is a malignant tumor originating from the bronchial mucosa or glands. Its morbidity and mortality rank first among malignant tumors and are increasing year by year. [0003] Early diagnosis and accurate clinical analysis of lung...

Claims

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Application Information

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IPC IPC(8): A61K51/06A61K103/34
Inventor 罗淑芳李娜张伟禄刘顺英余家会梁重时
Owner EAST CHINA NORMAL UNIVERSITY
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