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PH-responsive T1/T2 switching type MRI contrast agent as well as preparation method and application thereof

A contrast agent, switchable technology, applied in products, T1/T2 switchable MRI contrast agent and its preparation field, can solve the problem that the switchable contrast agent is rarely reported, and achieve enhanced high permeability and retention effect, improve imaging contrast, good biocompatibility

Active Publication Date: 2021-11-09
SUZHOU INST OF NANO TECH & NANO BIONICS CHINESE ACEDEMY OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Currently, such T 1 / T 2 Switching contrast agents have rarely been reported

Method used

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  • PH-responsive T1/T2 switching type MRI contrast agent as well as preparation method and application thereof
  • PH-responsive T1/T2 switching type MRI contrast agent as well as preparation method and application thereof
  • PH-responsive T1/T2 switching type MRI contrast agent as well as preparation method and application thereof

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preparation example Construction

[0046] Another aspect of the embodiment of the present invention also provides a pH response T 1 / T 2 Preparation method of switching MRI contrast agent, including:

[0047] A ring-containing polymerized polymerized reaction is carried out at least a first homogenate ring-containing mixed reaction system containing glutamate and propynamine to prepare a group-containing poly γ-benzyl-L-glutamic acid;

[0048] At least a reaction comprising the alkynyl group-containing poly γ-benzyl-L-glutamic acid is reacted with a second homogeneous mixed reaction system of the brominated acetic acetic acid solution to prepare a group-containing poly-L-glutamic acid;

[0049] At least the third uniform mixed reaction system containing the alkynyl group with 2-hydroxypyridine, a tertiary mixed reaction system of 2-hydroxypyridine, and a divinity, and is prepared to prepare a polyol-containing gauge {n- [N '- (2-aminoethyl) -2-aminoethyl] glutamate};

[0050] At least the polythynyl {N- [N- [N- (2...

Embodiment 1

[0104] A pH response T 1 / T 2 The preparation method of the switching MRI contrast agent (ESIONPS system) includes the following steps:

[0105] (1) Preparation of the allergy-containing poly γ-benzyl-L-glutamic acid: dichloromethane is stirred overnight by calcium hydride overnight and distilled to obtain a dry solution, dimethylformamide is dried over hydrogenated calcium and reduced pressure distillation The dried solution was obtained, and the glutamate chloride (BLG-NCA) was dissolved in a protective atmosphere in dichloromethane and dimethylformamide (volume ratio of 4: 1), and propargymine was added. 25 ° C reaction 24 h, where the molar ratio of the glutamic acid cyclic anhydride and the propargylamine is 40: 1, and the obtained solution is slowly added dropwise into the ice ether after the reaction is completed, and the solid is collected, dissolved in chlorine. EtOAc EtOAc EtOAc EtOAc,

[0106] (2) Preparation of the alkynyl group-containing poly-L-glutamic acid: alkyny...

Embodiment 2

[0119] A pH response T 1 / T 2 Preparation method of switching MRI contrast agent, including the following steps:

[0120] (1) Step (1) in Example 1, only the reaction time of glutamate chromataric anhydride (BLG-NCA) and the propargylamine were adjusted to 22 ° C for 36 h, and glutate benzyl ester The molar ratio of the rheinated acid anhydride and propargylamine is 50: 1;

[0121] (2) This step is similar to the step (2) in Example 1, and the alkynyl-containing poly γ-benzyl-glutamic acid is dissolved in trifluoroacetic acid trifluoroacetic acid in trifluoroacetate. In a 100 mL round bottom flask, a 33 wt% bromide solution was added, and then at 55 ° C for 3 h, it was reduced to a room temperature reaction for 18 h, resulting in a group-containing poly-L-glutamic acid;

[0122] (3) This step is similar to the step (3) in Example 1, only the alkynyl group-containing poly γ-benzyl-L-glutamic acid with 2-hydroxypyridine molar ratio of benzyl and 2-hydroxypyridine Adjusting to 1: 8,...

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Abstract

The invention discloses a pH-responsive T1 / T2 switching type MRI (Magnetic Resonance Imaging) contrast agent as well as a preparation method and application thereof. The T1 / T2 switching type MRI contrast agent has a structure shown in the following formula, wherein X is selected from 30-50, or m and n are selected from 30-50; and M is ferric oxide nanoparticles. The MRI contrast agent provided by the invention can specifically respond in a weak acid microenvironment of tumors, so that surface charges of contrast agent particles are changed, and aggregation of the ferric oxide nanoparticles is realized through electrostatic interaction, switching from a T1 contrast agent to a T2 contrast agent is realized, a T2 contrast enhancement effect is activated, and the MRI contrast agent has the advantages of high sensitivity and selectivity, low toxicity, good biocompatibility and the like in tumor diagnosis.

Description

Technical field [0001] In the field of pharmaceutical preparation of the present invention, specific to a pH response T 1 / T 2 Switching MRI contrast agent and its preparation method and application, for example, in the preparation of a product having tumor detection functions. Background technique [0002] Early diagnosis of cancer has important significance for cancer treatment. In many imaging imaging techniques, magnetic resonance imaging (MRI) is widely used in clinical diagnosis of tumors due to high spatial resolution, radiant injury and multi-directional scanning imaging. Since MRI technology has low sensitivity defects, it is sometimes difficult to distinguish between lesions and normal tissues in diagnosis, and thus usually introduce the contrast agent to solve this problem. The contrast agent commonly used in clinically is a tumor small molecular contrast agent, which can improve the contrast of tumors and normal tissues, but there is still a risk of renal systemic fi...

Claims

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Application Information

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IPC IPC(8): A61K49/12A61K49/18C08G83/00
CPCA61K49/126A61K49/1857C08G83/001
Inventor 裴仁军贺祎霖曹翼
Owner SUZHOU INST OF NANO TECH & NANO BIONICS CHINESE ACEDEMY OF SCI
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