Tumor-targeted diagnosis nuclear magnetic resonance contrast agent and preparation method thereof

A tumor targeting and nuclear magnetic resonance technology is applied in the field of nuclear magnetic resonance contrast agents, polypeptide-modified tumor-targeted diagnostic nuclear magnetic resonance contrast agents and their preparation, and tumor-targeted diagnostic nuclear magnetic resonance contrast agents and their preparation fields. Tumor targeted diagnosis of MRI contrast agent reports and other problems, to achieve the effect of high targeting and diagnosis efficiency, improving uptake, and avoiding interference

Inactive Publication Date: 2013-05-29
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

So far, there has been no report on MRI contrast agents for tumor-targeted diagnostics modified by peptides

Method used

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  • Tumor-targeted diagnosis nuclear magnetic resonance contrast agent and preparation method thereof
  • Tumor-targeted diagnosis nuclear magnetic resonance contrast agent and preparation method thereof
  • Tumor-targeted diagnosis nuclear magnetic resonance contrast agent and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0032] Take 3 mg polyamide-amine (PAMAM, 77.35 mg / ml methanol solution) and blow dry in a vial, add 3.64 mg polyethylene glycol (MAL-PEG3500-NHS, 1 mg / ml 0.035 M pH 8.0 phosphate solution) The molar ratio of the two is 1:10, and the reaction is stirred at room temperature for 2 h. The NHS group reacts specifically with the amino group on the surface of PAMAM to produce polyamide-amine-polyethylene glycol (PAMAM-PEG). 10 ) Complex solution, MWCO 5000 ultrafiltration centrifuge tube at 12000 rpm for 30 min to remove unreacted PEG, pH 7.0 phosphate buffer for reconstitution, add 0.52 mg T7 peptide (2 mg / ml pH 7.0 phosphate solution) , The molar ratio is 1:5, and the reaction is stirred at room temperature for 24 hours. The MAL group reacts specifically with the sulfhydryl group on the cysteine ​​residue of the T7 peptide to produce polyamide-amine-polyethylene glycol-polypeptide (PAMAM- PEG-T7) complex, MWCO 5000 ultrafiltration centrifuge tube at 12000 rpm for 30 min to remove unr...

Embodiment 2

[0034] Take 3 mg polyamide-amine (PAMAM, 77.35 mg / ml methanol solution) and blow dry in a vial, add 3.64 mg polyethylene glycol (MAL-PEG3500-NHS, 1 mg / ml 0.035 M pH 8.0 phosphate solution) The molar ratio of the two is 1:10, and the reaction is stirred at room temperature for 2 h. The NHS group reacts specifically with the amino group on the surface of PAMAM to produce polyamide-amine-polyethylene glycol (PAMAM-PEG). 10 ) Complex solution, MWCO 5000 ultrafiltration centrifuge tube with 12000 rpm ultrafiltration for 30 minutes to remove unreacted PEG, pH 9.0 phosphate buffer solution for reconstitution, and 13.4 mg bifunctional targeting ligand diethylenetriaminepentaacetic acid ( p-SCN-Bn-DTPA, 4 mg / ml pH 9.0 phosphate solution), molar ratio of 1:236, stirred at room temperature for 48 hours, SCN group reacts specifically with amino groups on the surface of PAMAM, and NMR imaging is obtained Reagent intermediate, MWCO 5000 ultrafiltration centrifuge tube was ultrafiltered at 120...

Embodiment 3

[0036] Take 3 mg polyamide-amine (PAMAM, 77.35 mg / ml methanol solution) and blow dry in a vial, add 3.64 mg polyethylene glycol (MAL-PEG3500-NHS, 1 mg / ml 0.035 M pH 8.0 phosphate solution) The molar ratio of the two is 1:10, and the reaction is stirred at room temperature for 2 h. The NHS group reacts specifically with the amino group on the surface of PAMAM to produce polyamide-amine-polyethylene glycol (PAMAM-PEG). 10 ) Complex solution, MWCO 5000 ultrafiltration centrifuge tube with 12000 rpm ultrafiltration for 30 minutes to remove unreacted PEG, pH 9.0 phosphate buffer solution for reconstitution, and 13.4 mg bifunctional targeting ligand diethylenetriaminepentaacetic acid ( p-SCN-Bn-DTPA, 4 mg / ml pH 9.0 phosphate solution), molar ratio of 1:236, stirred at room temperature for 48 hours, SCN group reacts specifically with amino groups on the surface of PAMAM, and NMR imaging is obtained Reagent intermediate, MWCO 5000 ultrafiltration centrifuge tube at 12000 rpm for 30 min ...

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Abstract

The invention belongs to the technical field of biotechnology, and relates to a tumor-targeted diagnosis nuclear magnetic resonance contrast agent and a preparation method thereof. The tumor-target diagnosis nuclear magnetic resonance contrast agent is prepared from a high molecular material, polyethylene glycol, a polypeptide, a dual-function ligand and gadolinium chloride by taking the polypeptide as a target head group, taking the tree-like high polymer material as a basic high molecular vector and connecting a small molecular contrast agent to the surface. In the invention, a polypeptide-modified high molecular material screened by using a phage display technology enters cells in an endocytic way, so that the introjection of the contrast agent by tumor cells is increased, and the characteristic of high safety is achieved. The target head group polypeptide used in the invention has the advantages of transferrin, can be used for effectively avoiding the interference of endogenous transferrin, has high targeting and diagnosing efficiencies, is simple to prepare, and can be further applied to target diagnosis of other tumor tissues.

Description

technical field [0001] The invention belongs to the field of biological technology, and relates to a nuclear magnetic resonance contrast agent, in particular to a tumor-targeted diagnosis nuclear magnetic resonance contrast agent and a preparation method thereof, in particular to a polypeptide-modified tumor-targeted diagnosis nuclear magnetic resonance contrast agent and a preparation method thereof. Background technique [0002] Diagnosis of tumors with magnetic resonance imaging and the study of highly effective contrast agents have attracted attention in recent years. At present, most of the contrast agents used clinically are hydrophilic small molecules, which cannot enter the cells, and often stay in the interstitial spaces and intravascular cavities through the vascular endothelial space. They are cleared quickly and cannot be imaged for a long time; Delivery only depends on the penetration of blood vessels into the tissue, resulting in the accumulation of contrast ag...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K49/14A61K49/12A61K103/34
Inventor 韩亮蒋晨黄容琴
Owner FUDAN UNIV
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