Tumor-targeted nonionic dendritic macromolecule magnetic resonance imaging contrast agent

A technology of dendritic macromolecules and magnetic resonance imaging, which is applied in the direction of nuclear magnetic resonance/magnetic resonance imaging contrast agents, preparations for in vivo experiments, pharmaceutical formulations, etc., can solve the problem of no biological specificity, lack of tissue selectivity, It is unfavorable for angiography and other problems, and achieves the effects of reducing drug dosage, reducing non-specific adsorption, and improving water solubility and biocompatibility

Inactive Publication Date: 2011-04-27
EAST CHINA NORMAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Although these contrast agents can meet some diagnostic requirements, they have some shortcomings, such as: due to the small size of the molecule, the osmotic pressure in the body is large, and it is easy to leak out from the blood vessel wall and enter the intercellular substance, so the metabolism in the body The rate is fast, which is not conducive to angiography; in addition, the distribution of small molecule contrast agents in the body has no biological specificity, lacks tissue selectivity, and is highly toxic to normal tissues

Method used

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  • Tumor-targeted nonionic dendritic macromolecule magnetic resonance imaging contrast agent
  • Tumor-targeted nonionic dendritic macromolecule magnetic resonance imaging contrast agent
  • Tumor-targeted nonionic dendritic macromolecule magnetic resonance imaging contrast agent

Examples

Experimental program
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Effect test

Embodiment 1

[0035] a)H 2 Synthesis of N-PEG2000-FA

[0036] Take NH2 -PEG2000-NH 2 (1.0g, 0.5mmol), FA (0.22g, 0.5mmol), DCC (0.12g, 0.6mmol) were dissolved in 10mL DMSO, added 20μL pyridine, at room temperature, N 2 Protection stirring reaction 48h. The reaction solution was diluted with 10 mL of deionized water, filtered to remove the by-product DCU, and the filtrate was dialyzed in deionized water for 72 hours with a molecular weight cut-off of 1000, then freeze-dried, and finally purified with a silica gel column to obtain H 2 N-PEG2000-FA, 65% yield.

[0037] b) Synthesis of SuO-DTPA-PEG2000-FA

[0038] Suspend DTPAA (1.0g, 2.8mmoL) in 10mL dry DMF, add NHS (0.65g, 5.6moL) and a catalytic amount of DMAP at 70°C under stirring, stir the reaction at this temperature for 4h, cool to room temperature, pour into In 150 mL of isopropanol, the solid was filtered out, washed with absolute ethanol and ether, and dried in vacuo to obtain a white powdery solid SuO-DTPA-SuO with a yield of ...

Embodiment 2

[0046] The preparation process was the same as that in Example 1. The molecular weight of PEG was fixed at 2000, and the generation number of PAMAM was changed to synthesize PAMAM-DTPA-PEG-FA / Gd of the 3.0th generation, 4.0th generation, and 5.0th generation respectively.

Embodiment 3

[0048] The preparation process was the same as in Example 1. The generation number of PAMAM was fixed, and the molecular weight of PEG was changed. The dendrimer contrast agent was synthesized with molecular weights of 1000, 2000, and 4000 respectively. It was found that the particle size of nanoparticles increased significantly with the molecular weight of PEG.

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Abstract

The invention discloses a tumor-targeted nonionic dendritic macromolecule magnetic resonance imaging contrast agent and a preparation method thereof. The contrast agent is a spherical nano composite particle prepared by taking a PAMAM dendritic macromolecule as a nuclear, folic acid as a targeting group, polyethyleneglycols (PEG) with different molecular weights as linking arms between the targeting group and a macromolecular carrier, and diethylenetriamine pentaacetic acid (DTPA) as a Gd<3+> ligand; and the preparation method comprises the following steps: reacting H2N-PEG-FA with folic acidresidue and diethylenetriamine pentaacetic acid double active ester (SuO-DTPA-SuO) to obtain SuO-DTPA-PEG-FA; and then bonding the SuO-DTPA-PEG-FA on the surface of the PAMAM to obtain PAMAM-DTPA-PEG-FA; and finally chelating the PAMAM-DTPA-PEG-FA and Gd<3+>. The imaging contrast agent prolongs the circulation time in blood, improves the relaxation rate, can be effectively distributed in tumor tissues, reduces the toxicity on normal tissues, and has the advantages of long-acting circulation in vivo, improvement of the relaxation rate, reduction of the medicament consumption and the like.

Description

technical field [0001] The invention relates to a magnetic resonance imaging contrast agent, in particular to a non-ionic polyamide-amine (PAMAM) dendrimer magnetic resonance imaging contrast agent targeted at tumors and capable of long-lasting circulation in blood and a preparation method thereof. technical background [0002] Magnetic resonance imaging (MRI) technology is one of the new technologies in medical imaging diagnostics. It uses different magnetic resonance signals generated by different tissues in the body under the influence of an external magnetic field for imaging. In clinical applications, more than 30% of diagnostics use To MRI contrast agent (MRIcontrast agent). Contrast agents can shorten the relaxation time of protons and enhance the contrast of magnetic resonance signals between normal tissues and diseased tissues, thereby improving the clarity of images. The contrast agents commonly used in clinical practice are all small molecule contrast agents, suc...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K49/06A61K49/12
Inventor 余家会段孔荣唐晓星刘彦运刘顺英罗淑芳
Owner EAST CHINA NORMAL UNIV
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