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Superparamagnetic particles targeting rheumatoid arthritis part as well as preparation method and application of particles

A superparamagnetic and rheumatoid technology, applied in preparations for in vivo tests, pharmaceutical formulations, MRI/MRI contrast agents, etc., can solve the problem of poor specificity of Gd-based contrast agents and the ability of joint-targeted imaging Insufficient and other problems, to achieve the effect of improving imaging ability and signal-to-noise ratio, and improving targeting ability

Active Publication Date: 2014-04-02
INST OF PROCESS ENG CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In the imaging of rheumatoid arthritis, Gd-based contrast agents have some obvious disadvantages: First, small molecule Gd-based contrast agents have poor specificity
However, most of the existing contrast agents are suitable for lymphatic or liver-targeted imaging, and their ability to target joint imaging is insufficient. It is often necessary to increase the dose of contrast agent to reach 20mg / kg body weight to achieve contrast.

Method used

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  • Superparamagnetic particles targeting rheumatoid arthritis part as well as preparation method and application of particles
  • Superparamagnetic particles targeting rheumatoid arthritis part as well as preparation method and application of particles

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0067] (1) Activation of folic acid: Dissolve 0.45g of folic acid and 0.21g of DCC in 10.6mL of anhydrous DMSO, and react for 6 hours in the dark;

[0068] (2) Preparation of superparamagnetic particle suspension: take 90 mg of superparamagnetic particles, disperse them in 9 mL of anhydrous DMSO, and keep the final concentration at 1 mg / mL;

[0069] (3) Add the suspension prepared in step (2) to the solution obtained in step (1), and add 12.9 mg of DMAP, and react for 6 hours at room temperature;

[0070] (4) Separation: After the reaction, centrifuge at 5000 rpm / min for 30 min to obtain the product and redisperse it in PBS to obtain the desired contrast agent.

[0071] Wherein (2) the preparation method of the superparamagnetic particle is as follows: the iron acetylacetonate (Fe(acca) 3 ) and 1 g of PEG550-b-PAA1000 were dissolved in triethylene glycol, and the solution was stirred under the protection of an inert gas while heating to 160°C and refluxed, then heating soluti...

Embodiment 2

[0073] (1) Activation of folic acid: Dissolve 4.5g of folic acid and 2.1g of DCC in 10.6mL of anhydrous DMSO, and react for 6 hours in the dark;

[0074] (2) Preparation of superparamagnetic particle suspension: take 900 mg of superparamagnetic particles, disperse them in 9 mL of anhydrous DMSO, and keep the final concentration at 10 mg / mL;

[0075] (3) Add the suspension prepared in step (2) to the solution obtained in step (1), and add 129 mg of DMAP, and react for 6 hours at room temperature;

[0076] (4) Separation: After the reaction, centrifuge at 5000 rpm / min for 30 min to obtain the product and redisperse it in PBS to obtain the desired contrast agent.

[0077] Wherein (2) the preparation method of the superparamagnetic particle is as follows: the iron acetylacetonate (Fe(acca) 3 ) and 1 g of PEG550-b-PAA1000 were dissolved in triethylene glycol, and the solution was stirred under the protection of an inert gas while heating to 160°C and refluxed, then heating solutio...

Embodiment 3

[0079] (1) Activation of folic acid: Dissolve 4.5g of folic acid and 2.1g of DCC in 10.6mL of anhydrous DMSO, and react for 18 hours in the dark;

[0080] (2) Preparation of superparamagnetic particle suspension: take 900 mg of superparamagnetic particles, disperse them in 9 mL of anhydrous DMSO, and keep the final concentration at 10 mg / mL;

[0081] (3) Add the suspension prepared in step (2) to the solution obtained in step (1), and add 129 mg of DMAP, and react for 18 hours at room temperature;

[0082] (4) Separation: After the reaction, centrifuge at 5000 rpm / min for 30 min to obtain the product and redisperse it in PBS to obtain the desired contrast agent.

[0083] Wherein (2) the preparation method of the superparamagnetic particle is as follows: the iron acetylacetonate (Fe(acca) 3 ) and 1 g of PEG550-b-PAA1000 were dissolved in triethylene glycol, and the solution was stirred under the protection of an inert gas while heating to 160°C and refluxed, then heating solut...

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Abstract

The invention provides a contrast medium capable of developing rheumatoid arthritis parts in magnetic resonance imaging for realizing targeted developing by utilizing high affinity of folate and macrophages with folate receptors expressed on the surface. The magnetic resonance contrast medium is prepared by adopting a chemical connection method (namely dicyclohexylcarbodiimide / 4-dimethylamino-pyridine method, DCC / DMAP method). The method comprises the following step: coupling polyethylene glycol(PEG)-b-polyacrylic acid (PAA) modified superparamagnetic particles with folate molecule to obtain the magnetic resonance imaging contrast medium which has the particle size of about 20nm, is high in specificity and good in contrast effect and is used for imaging rheumatoid arthritis parts.

Description

technical field [0001] The present invention relates to a superparamagnetic particle with rheumatoid arthritis site-targeting effect and a preparation method thereof, and also relates to a superparamagnetic magnetic particle containing the superparamagnetic particle specifically targeting at the site of rheumatoid arthritis. Resonance contrast agent and its preparation method. Background technique [0002] Magnetic resonance imaging (MRI) is one of the most widely used imaging methods at present. In clinical MRI detection, more than 30% of the diagnoses require MRI contrast agents to improve imaging contrast, so that the original lack of contrast difference tissue The structure is displayed more clearly, so as to better display the structure of tissues and organs in the body and the nature and functional status of lesions, which can greatly improve the accuracy and early diagnosis. [0003] MRI contrast agents can be divided into positive and negative contrast agents accord...

Claims

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Application Information

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IPC IPC(8): A61K49/18A61K49/10A61K49/12A61K49/08
Inventor 张欣代凤英钟砚琦何艳刘颖果
Owner INST OF PROCESS ENG CHINESE ACAD OF SCI