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Optical three-mode targeted contrast agent for lung non-cellule cancer as well as preparation method and application thereof

A non-small cell cancer, targeted contrast agent technology, applied in the direction of X-ray contrast agent preparation, general/multifunctional contrast agent, pharmaceutical formulations, etc., can solve the problem of non-small cell carcinoma of the lung not found in contrast performance and other issues

Active Publication Date: 2016-08-24
SHANGHAI FIRST PEOPLES HOSPITAL +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0010] A search of domestic and foreign literature and patents on the use of gold nanoparticles in CT / MR / optical three-mode imaging found that: before the completion of the present invention, no lung non-small cell based on Cy5.5-Gd-Au DENPs-FA has been found. Preparation of cancer CT / MR / near-infrared optical three-modal targeting contrast agent and its contrast performance research

Method used

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  • Optical three-mode targeted contrast agent for lung non-cellule cancer as well as preparation method and application thereof
  • Optical three-mode targeted contrast agent for lung non-cellule cancer as well as preparation method and application thereof
  • Optical three-mode targeted contrast agent for lung non-cellule cancer as well as preparation method and application thereof

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0074] First, FA-PEG-COOH was synthesized according to previous studies.

[0075] Take the fifth generation polyamide-amine dendrimers (G5.NH 2 ) 81.47mg, dissolved in 20mL DMSO to obtain a solution, then DOTA-NHS (23.85mg) dissolved in DMSO (10mL) was added dropwise to the above solution, and stirred with strong magnetic force for 24h to obtain G5.NH2-DOTA. FA-PEG-COOH (61.04 mg) was activated by EDC (1-ethyl-(3-dimethylaminopropyl) carbodiimide hydrochloride) (48.04 mg dissolved in 10 mL DMSO) for 3 hours, and gradually Add G5.NH dropwise 2 -DOTA solution, followed by strong magnetic stirring for 3 days, the obtained G5.NH2-DOTA-(PEG-FA) was further modified by mPEG-COOH (93.96 mg) that had been activated by EDC for 3 hours, and G5 was obtained after magnetic stirring for 3 days .NH 2 -DOTA-(PEG-FA)-mPEG dendrimer.

[0076] Such as figure 2 as shown, 1 H NMR spectrum proves that mPEG-COOH has been successfully modified in G5.NH 2 On the surface of the dendrimer, each...

Embodiment 2

[0078] With the G5.NH in embodiment 1 2 -DOTA-(PEG-FA)-mPEG dendrimers were further modified with 3 molar equivalents of Cy5.5 (6.73 mg) and stirred under strong magnetic force for 1 h in the dark to obtain G5.NH 2 -DOTA-(PEG-FA)-mPEG-Cy5.5.

[0079] Such as image 3 As shown, the absorption peak at 650nm in the ultraviolet spectrum is the absorption peak of Cy5.5, which proves that Cy5.5 is successfully conjugated on the surface of the dendrimer.

Embodiment 3

[0081] Get the G5.NH prepared in Example 2 2 -DOTA-(PEG-FA)-mPEG-Cy5.5 dendrimer solution, add 5.72 mL (30 mg / mL) of chloroauric acid solution, and stir for 30 minutes. Then add frozen sodium borohydride solution (78.98mg, 10mL) loaded with more than 5 times the mole of gold particles, and stir for several minutes until the color of the reaction mixture turns to wine red, suggesting that the gold nanoparticles have been synthesized on the macromolecules. The reaction mixture was stirred for 2 h to complete the reaction. After that, the Gd(NO 3 ) 3 Aqueous solution (32.80 mg, 1 mL) and 35 molar equivalents of G5 dendrimers were added dropwise to the above mixture, stirred for 24 h to obtain {(Au°)200-G5.NH 2 -DOTA(Gd)-(PEG-FA)-mPEG-Cy5.5}DENPs.

[0082] After the reaction, 160.0 uL of triethylamine was added, and magnetically stirred for 30 min, then, 130.3 uL of acetic anhydride was added, and the reaction was stirred for 24 h. After the reaction, the reaction mixture was...

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Abstract

The invention relates to a CT / MR / near infrared optical three-mode targeted contrast agent based on the lung non-cellule cancer as well as a preparation method and application thereof. The preparation method comprises the following steps: firstly, modifying the amino terminal of a fifth-generation polyamide-amine dendrimer with DOTA-NHS; secondly, connecting folic acid to the dendrimer by polyethylene glycol; thirdly, further modifying with Cy5.5; fourthly, preparing gold nanoparticles by using the modified dendrimer as a template through sodium borohydride reduction, and chelating gadolinium ions to the dendrimer; fifthly, carrying out complete acetylization on amino remained on the surface of the dendrimer; and finally, dialyzing the reacted solution, lyophilizing to obtain a final product, and evaluating in-vivo and in-vitro CT / MR / near infrared optical three-mode contrast performance of the product. The method is simple and feasible, has excellent in-vivo and in-vitro lung non-cellule cancer cell target effect, and has a potential application prospect of targeted CT / MR / near infrared optical contrast.

Description

technical field [0001] The invention belongs to the field of preparation of contrast agents, in particular to a method for preparing a Cy5.5-Gd-Au DENPs-FA-based three-mode targeting contrast agent for lung non-small cell carcinoma CT / MR / near-infrared optics. Background technique [0002] In research and clinical applications, many imaging modalities have been widely used, such as CT, MR, near-infrared optical imaging, PET, SPECT. Among these modalities, CT offers better spatial and density resolution than other imaging modalities, and MR imaging offers superior soft-tissue contrast, high spatial resolution, and flexible sectioning capabilities. Although optical imaging is inferior in resolution to CT or MR, optical imaging provides good detection sensitivity. Since these imaging modes have their own advantages and disadvantages, the joint application of these modes will get more ideal results. [0003] Nanomedicine opens a new avenue for molecular imaging, which can provi...

Claims

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Application Information

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IPC IPC(8): A61K49/00A61K49/04A61K49/18
CPCA61K49/0002A61K49/0065A61K49/0423A61K49/1851
Inventor 王悍陈静文史向阳程潜
Owner SHANGHAI FIRST PEOPLES HOSPITAL
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