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

A tumor targeting and nuclear magnetic resonance technology, which is applied in the tumor targeted diagnosis nuclear magnetic resonance contrast agent and its preparation, the polypeptide-modified tumor targeted diagnosis nuclear magnetic resonance contrast agent and its preparation, and the field of nuclear magnetic resonance contrast agent, which can solve the problems that have not yet been seen. Tumor targeted diagnosis of MRI contrast agent reports and other issues, to achieve high targeting and diagnosis efficiency, avoid interference, and improve the effect of uptake

Inactive Publication Date: 2012-04-04
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
Comparison scheme
Effect test

Embodiment 1

[0033] Take 3 mg of polyamidoamine (PAMAM, 77.35 mg / ml methanol solution) and dry it 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, and the NHS group reacts specifically with the amino group on the surface of PAMAM to make polyamide-amine-polyethylene glycol (PAMAM-PEG 10) complex solution, MWCO 5000 ultrafiltration centrifuge tube at 12000 rpm for 30 min to remove unreacted PEG, redissolve in pH 7.0 phosphate buffer, add 0.52 mg T7 peptide (2 mg / ml pH 7.0 phosphate solution) , with a molar ratio of 1:5, stirred at room temperature for 24 h, and the MAL group reacted specifically with the sulfhydryl group on the cysteine ​​residue of the T7 peptide to produce a polyamide-amine-polyethylene glycol-polypeptide (PAMAM- PEG-T7) complex, MWCO 5000 ultrafiltration centrifuge tube at 12000 rpm for 30 min to remove unreacted T7 peptide...

Embodiment 2

[0035] Take 3 mg of polyamidoamine (PAMAM, 77.35 mg / ml methanol solution) and dry it 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, and the NHS group reacts specifically with the amino group on the surface of PAMAM to make polyamide-amine-polyethylene glycol (PAMAM-PEG 10 ) complex solution, MWCO 5000 ultrafiltration centrifuge tube at 12000 rpm for 30 min to remove unreacted PEG, reconstituted in pH 9.0 phosphate buffer, and 13.4 mg bifunctional targeting ligand diethylenetriaminepentaacetic acid ( p-SCN-Bn-DTPA, 4 mg / ml pH 9.0 phosphate solution), the molar ratio was 1:236, stirred at room temperature for 48 h, the SCN group reacted specifically with the amino group on the surface of PAMAM, and obtained NMR Reagent intermediate, MWCO 5000 ultrafiltration centrifuge tube at 12000 rpm for 30 min to remove unreacted bifunctional...

Embodiment 3

[0037] Take 3 mg of polyamidoamine (PAMAM, 77.35 mg / ml methanol solution) and dry it 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, and the NHS group reacts specifically with the amino group on the surface of PAMAM to make polyamide-amine-polyethylene glycol (PAMAM-PEG 10 ) complex solution, MWCO 5000 ultrafiltration centrifuge tube at 12000 rpm for 30 min to remove unreacted PEG, reconstituted in pH 9.0 phosphate buffer, and 13.4 mg bifunctional targeting ligand diethylenetriaminepentaacetic acid ( p-SCN-Bn-DTPA, 4 mg / ml pH 9.0 phosphate solution), the molar ratio was 1:236, stirred at room temperature for 48 h, the SCN group reacted specifically with the amino group on the surface of PAMAM, and obtained NMR Reagent intermediate, MWCO 5000 ultrafiltration centrifuge tube at 12000 rpm for 30 min to remove unreacted bifunctional...

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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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IPC IPC(8): A61K49/14A61K49/12A61K103/34
Inventor 韩亮蒋晨黄容琴
Owner FUDAN UNIV
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