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Preparation of CT/MR bimodal imaging nano contrast medium with folate targeting function

A dual-modality imaging and nano-contrast agent technology, which is used in preparations for in vivo experiments, pharmaceutical formulations, etc.

Inactive Publication Date: 2012-09-19
DONGHUA UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] A search of domestic and foreign literature and patents on CT / MRI dual-modality contrast agents shows that no folic acid-modified dendrimers coated with gold nanoparticles have been used for targeted CT / MRI dual-modality imaging nanoparticles. Contrast media reports

Method used

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  • Preparation of CT/MR bimodal imaging nano contrast medium with folate targeting function
  • Preparation of CT/MR bimodal imaging nano contrast medium with folate targeting function
  • Preparation of CT/MR bimodal imaging nano contrast medium with folate targeting function

Examples

Experimental program
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Effect test

Embodiment 1

[0059] (1) Dilute 39 mg of folic acid with 20 mL of dimethyl sulfoxide solution, activate with 169 mg of EDC for 3 hours, then add polyethylene glycol (88.40 mg dry weight) dissolved in 1 mL of dimethyl sulfoxide drop by drop while stirring ( NH 2 -PEG-COOH), after reacting for 70~80h, the reaction product was dialyzed in the buffer solution with a dialysis membrane for 24h, then dialyzed with distilled water for 48h, and finally the purified product was freeze-dried to obtain a folic acid-modified polyethylene glycol solid product ( FA-PEG-COOH);

[0060] (2) Dissolve the 5th generation polyamide-amine type (PAMAM) dendrimers with a dry weight of 30 mg in 15 mL of dimethyl sulfoxide solution, and then add the dry weight dissolved in 5 mL of dimethyl sulfoxide solution dropwise while stirring. 8.83 mg of DOTA-NHS, reacted for 24 hours, then took 22.49 mg of FA-PEG-COOH obtained in (1), dissolved in 5 mL of dimethyl sulfoxide solution and activated with EDC, added dropwise to ...

Embodiment 2

[0064] (1) Dilute 29 mg of folic acid with 20 mL of dimethyl sulfoxide solution, activate with 125.67 mg of EDC for 3 hours, then add polyethylene glycol with a dry weight of 65.73 mg dissolved in 1 mL of dimethyl sulfoxide drop by drop while stirring (NH 2 -PEG-COOH), after reacting for 70~80h, the reaction product was dialyzed in the buffer solution with a dialysis membrane for 24h, then dialyzed with distilled water for 48h, and finally the purified product was freeze-dried to obtain a folic acid-modified polyethylene glycol solid product ( FA-PEG-COOH);

[0065] (2) Dissolve the 5th generation polyamide-amine type (PAMAM) dendrimers with a dry weight of 20 mg in 15 mL of dimethyl sulfoxide solution, and then add the dry weight dissolved in 5 mL of dimethyl sulfoxide solution dropwise while stirring. 5.89 mg of DOTA-NHS, reacted for 24 hours, then took 14.99 mg of FA-PEG-COOH obtained in (1), dissolved in 5 mL of dimethyl sulfoxide solution and activated with EDC, added dr...

Embodiment 3

[0069] In order to study the material {(Au 0 ) 200 –G5.NHAc-DOTA (GdⅢ) 10 -PEG 11 -FA 5}DENPs and materials{(Au 0 ) 200 –G5.NHAc-DOTA 10 -PEG 11 The X-ray absorption and CT imaging effects of -FA5}DENPs were demonstrated by using in vitro CT imaging and calculating the HU value by measurement. Take {(Au 0 ) 200 –G5.NHAc-DOTA (GdⅢ) 10 -PEG 11 -FA 5}DENPs 20.29 mg was dissolved in 1000 μL PBS solution, and the concentration of gold nanoparticles was prepared to be 0.08M. After a series of dilutions, 200 μL of PBS solutions with gold concentrations of 0.05, 0.04, 0.02, and 0.01M were formed; the same was used for the comparison 1 in {(Au 0 ) 200 -G5.NHAc-DOTA 10 -PEG 11 -FA 5}DENPs 20.61 mg was dissolved in 1000 μL PBS solution, and the concentration of gold nanoparticles was prepared to be 0.08 M. After a series of dilutions, 200 μL of PBS solutions with gold concentrations of 0.05, 0.04, 0.02, and 0.01 M were formed. Tested by CT scan (attached Figure 5 ), i...

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Abstract

The invention relates to a preparation method of a CT / MR bimodal imaging nano contrast medium with a folate targeting function. The method comprises the following steps of: (1) preparing FA-PEG-COOH; (2) modifying the dendrimer by use of DOTA-NHS, COOH-PEG-FA and mPEG-COOH to obtain the pegylation dendrimer modified by DOTA and folate; and (3) adding chloroauric acid solution, NaBH4 solution and Gd(NO3)3.6H2O into the dendrimer solution obtained in the step (2), then adding triethylamine and acetic anhydride, and after reaction, performing dialysis and freeze-drying. The preparation method provided by the invention is simple and easy to operate, and has mild reaction conditions and prospects for industrial implementation; and the CT / MR bimodal imaging nano contrast medium has better water solubility and stability, realizes a specific targeting function for the folate receptor high-expression cancer cell, and is expected to be applied to early detection of tumor.

Description

technical field [0001] The invention belongs to the field of preparation of CT / MR dual-mode imaging nano-contrast agent, in particular to a preparation method of CT / MR dual-mode imaging nano-contrast agent with folic acid targeting function. Background technique [0002] Cancer has become one of the main killers that endanger human health all over the world, and the earlier cancer is detected, the higher the possibility of cure. Studies have shown that if cancer can be detected early, 30% of cancer patients will survive (Action Plan for the Global Strategy for the Prevention and Control of Noncommu-nicable Diseases. World Health Organization, 2008, 2008–2013http: / / www. who.int / nmh / publica-tions / 9789241597418 / en / index.html). Therefore, the development of early detection technology of cancer is the key to overcoming cancer treatment. CT imaging and MR imaging are commonly used in clinical diagnosis of cancer, and they have high spatial resolution, so they have been extensive...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K49/10A61K49/12
Inventor 史向阳陈潜温诗辉李康安张贵祥
Owner DONGHUA UNIV
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