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Iodine-containing nanoparticles for tumor-targeted CT imaging and preparation method thereof

A tumor-targeting, nanoparticle-based technology, applied in the field of preparation of iodine-containing nanoparticle contrast agents, to achieve the effects of strong controllability, long circulation time in the body, and good biocompatibility

Active Publication Date: 2020-12-22
TIANJIN MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the EPR effect is a passive targeting process, and it is difficult to achieve effective accumulation of nanoparticles in tumor sites.

Method used

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  • Iodine-containing nanoparticles for tumor-targeted CT imaging and preparation method thereof
  • Iodine-containing nanoparticles for tumor-targeted CT imaging and preparation method thereof
  • Iodine-containing nanoparticles for tumor-targeted CT imaging and preparation method thereof

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Experimental program
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Embodiment 1

[0043] Step 1: Add 10.0 g of iopamidol (substance II) and 0.520 g of concentrated sulfuric acid to 40 mL of anhydrous N,N-dimethylacetamide, and then add the hydroxyl protecting agent 2,2-dimethylacetamide dropwise under stirring 6.40 mL of oxypropane was added to keep the reaction temperature at about 55 °C, and the reaction was stopped after stirring for 24 h. The reaction solution was neutralized with 3% sodium bicarbonate solution, and most of the solvent was removed by rotary evaporation to obtain a light yellow oil. 150 mL of distilled water was added to the oil, stirred at room temperature for 2 h, and then centrifuged to obtain a white solid, which was washed twice with distilled water to remove unreacted raw materials and impurities. The resulting product was dried in a vacuum oven at 50°C to obtain 8.0 g of crude product, which was separated and purified by silica gel column chromatography (dichloromethane:methanol=15:1) to obtain 5 g of white compound III, the final...

Embodiment 2

[0055] Step 1: Add 10.0 g of iopamidol (substance II) and 0.520 g of concentrated sulfuric acid to 40 mL of anhydrous N,N-dimethylacetamide, then add 2,2-dimethoxypropane dropwise under stirring 6.40 mL, the reaction temperature was maintained at about 55 °C, and the reaction was stopped after stirring for 24 h. The reaction solution was neutralized with 3% sodium bicarbonate solution, and most of the solvent was removed by rotary evaporation to obtain a light yellow oil. 150 mL of distilled water was added to the oil, stirred at room temperature for 2 h, and then centrifuged to obtain a white solid, which was washed twice with distilled water to remove unreacted raw materials and impurities. The resulting product was dried in a vacuum oven at 50°C to obtain 8.0 g of crude product, which was separated and purified by silica gel column chromatography (dichloromethane:methanol=15:1) to obtain 5 g of white compound III, the final yield was 45.6%. product by 1 H-NMR, MS and FTI...

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Abstract

The invention relates to preparation and application of a nanometer contrast agent for tumor targeted CT imaging. The nanometer contrast agent having a tumor targeted CT imaging function is prepared by the following steps: firstly, designing and synthesizing an iodine-containing functional monomer compound which can be applied to polymerization based on a clinically-used small molecular CT contrast agent, namely, iopamidol; then, preparing iodine-containing polymer nanoparticles with appropriate particle sizes by precipitation polymerization, and performing polyethylene glycol and RGD peptidesurface modification on the iodine-containing polymer nanoparticles. The prepared iodine-containing nanoparticles can be used as a contrast agent for tumor CT imaging, so that a reliable theoretical basis and a method basis are laid for highly-sensitive diagnosis of tumors.

Description

technical field [0001] The invention relates to an iodine-containing nanoparticle for tumor-targeted CT imaging and a preparation method thereof, in particular to a preparation method and clinical application of an iodine-containing nanoparticle contrast agent for tumor-targeted CT imaging . Background technique [0002] Malignant tumors rank first in the cause of death in my country. Some cancers are difficult to diagnose due to the lack of obvious early symptoms. Once symptoms appear, most of the disease course has entered the middle and late stages. Therefore, early and accurate diagnosis of tumors is very important. At present, the early diagnosis of clinical tumors mainly relies on positron emission tomography-X-ray computed tomography (PET-CT), that is, human metabolites such as glucose labeled with radioactive positron nuclides are used as contrast agents, and high metabolism Due to the high uptake performance of this contrast agent, the location of the tumor can be...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K49/04
CPCA61K49/049
Inventor 杨晓英高春会张瀛化王利邢超王银松陈研
Owner TIANJIN MEDICAL UNIV
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