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Preparation of diatrizoic-acid-modified double-element target CT (Computed Tomography) contrast agent containing gold and iodine

A pan-diatrizoic acid and contrast agent technology, which is used in the preparation of X-ray contrast agents, can solve the problems of limited gold loading, and does not involve the preparation of targeted imaging contrast agents, and achieves good biocompatibility and water-solubility. Effect

Inactive Publication Date: 2012-10-03
DONGHUA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, in these previous works, on the one hand, the uploading amount of gold was relatively limited (Au:G5.NH 2 =50:1), the imaging sensitivity needs to be improved; on the other hand, the above work does not involve the preparation of targeted imaging contrast agents
[0005] Summarizing the current research findings, there are no literature reports or patent applications for CT contrast agents that contain both gold and iodine imaging elements and have targeting functions.

Method used

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  • Preparation of diatrizoic-acid-modified double-element target CT (Computed Tomography) contrast agent containing gold and iodine
  • Preparation of diatrizoic-acid-modified double-element target CT (Computed Tomography) contrast agent containing gold and iodine
  • Preparation of diatrizoic-acid-modified double-element target CT (Computed Tomography) contrast agent containing gold and iodine

Examples

Experimental program
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Effect test

Embodiment 1

[0067] 30eq each time (with G5.NH 2 The molar ratio, the same below) of chloroauric acid is added to the fifth generation polyamidoamine dendrimers (G5.NH 2 ) aqueous solution, stirred for 10min, then added 150eq of NaBH 4 Reduction, after continuous stirring for 30 minutes, add 150eq of HCl and NaOH (both 0.3mol / L) to adjust the pH of the solution to be neutral, then repeat the above process 3 times until 120eq of gold is uploaded into the dendrimer, the reaction Control G5.NH 2 The concentration is about 1mg / mL. Finally, the Au NPs solution was obtained by dialysis with PBS and deionized water respectively. The molecular weight cut-off of the regenerated cellulose dialysis bag used was MWCO=14000, and the reaction in Example 2 was continued without drying.

Embodiment 2

[0069] Dissolve 200eq of diatrizoic acid (DTA) in dimethylsulfoxide (DMSO), 1000eq of 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (EDC.HCl ) and 1000eq of N-hydroxysulfosuccinimide (NHS) were also dissolved in DMSO, firstly add EDC to the DTA solution and stir for 2h, then add NHS and continue stirring for 2h to activate the carboxyl group on DTA, and finally activate The good DTA solution was added drop by drop into the dialyzed Au NPs aqueous solution in (1), control DMSO: water = 1:4 (v:v), keep stirring for 3 days, and then use PBS with pH=7.4 Buffer dialysis for 1 day (3 times, 4 liters / time), and then deionized water dialysis for 1 day (3 times, 4 liters / time), to obtain {(Au 0 ) 120 -G5.NH 2 The nanocomposite of -DTA}, need not dry to continue the reaction of embodiment 3;

Embodiment 3

[0071] The FA-PEG-COOH of 10eq and the mPEG-COOH of 10eq were sequentially mixed with {(Au 0 ) 120 -G5.NH 2 -DTA} nanoparticle reaction, in the experiment, EDC.HCl and NHS were all dissolved in water, COOH-PEG-FA and mPEG-COOH were activated in the aqueous phase system, and then added to {(Au 0 ) 120 -G5.NH 2 -DTA} in aqueous solution, respectively reacted for 3 days, and then used acetic anhydride in the presence of triethylamine to acetylate all the remaining amino groups on the surface of the dendrimer, then dialyzed with PBS and deionized water respectively, and freeze-dried to obtain Solid product {(Au 0 ) 120 -G5.NHAc-DTA 30 -(PEG-FA) 6-mPEG 9} DSNPs.

[0072] Wherein the obtained gold nanoparticles of each step are tested with a UV-Vis spectrometer after dialysis, and the surface plasmon resonance peak of the gold nanoparticles can be clearly seen at about 524nm (attached figure 1 ), and its particle size and shape changes were tested by TEM (attached Figure...

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Abstract

The invention relates to a preparation method of a diatrizoic-acid-modified double-element target CT (Computed Tomography) contrast agent containing gold and iodine. The preparation method comprises the following steps of: (1) adopting a fifth-generation polyamide-amine dendroid macromolecule as a template, adopting a gradual reduction method to load higher-content gold nanoparticles and forming Au NPs; (2) connecting small-molecular diatrizoic-acid containing the iodine onto the amino group of the surface of the dendroid macromolecule by EDC activation action to obtain the nano compound containing gold and iodine simultaneously; and (3) connecting carboxylic polyethylene glycol-folic acid and methoxy polyethylene glycol onto the surface of the nano compound in the step (2) sequentially by EDC activation action, and finally under the existence of triethylamine, acetylizing all the remained amino groups on the surface of the dendroid macromolecule by using acetic anhydride, dialyzing, and freeze-drying to obtain the diatrizoic-acid-modified double-element target CT contrast agent containing the gold and the iodine. The preparation method is simple in operation, mild in condition and easy in operation; and the CT contrast agent is good in imaging effect and has the advantages of good water solubility and biocompatibility.

Description

technical field [0001] The invention belongs to the field of preparation of targeted CT contrast agents, in particular to a preparation method of a dual-element targeted CT contrast agent containing gold and iodine modified with diatrizoic acid. Background technique [0002] Due to its high spatial resolution, computed tomography (CT) imaging technology is convenient and effective. It has been widely used in the early diagnosis and treatment of various diseases, especially cancer. In order to enhance the effect of CT imaging, To achieve satisfactory imaging quality, contrast agents become very necessary. Traditional CT imaging agents are usually some iodine-containing small molecule compounds, such as: iohexol, iodized oil, iopanoic acid and diatrizoic acid, etc. These small molecule imaging agents have many disadvantages, and their blood circulation time is short, Imaging time is short, and it lacks specificity, and it cannot perform targeted imaging on tissues. At the sam...

Claims

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Application Information

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IPC IPC(8): A61K49/04C08G81/00
Inventor 史向阳肖婷婷彭琛
Owner DONGHUA UNIV
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