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MRI contrast agent taking chitosan derivative as carrier and preparation method

A technology of chitosan derivatives and contrast agents, applied in the field of medical clinical magnetic resonance imaging, can solve the problems of slow excretion of macromolecules and limit the application, and achieve the effects of easy control, high relaxation rate and good biocompatibility

Active Publication Date: 2016-11-23
SUZHOU INST OF NANO TECH & NANO BIONICS CHINESE ACEDEMY OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, due to the slow excretion of macromolecules in the body, its clinical application is limited.

Method used

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  • MRI contrast agent taking chitosan derivative as carrier and preparation method
  • MRI contrast agent taking chitosan derivative as carrier and preparation method
  • MRI contrast agent taking chitosan derivative as carrier and preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Embodiment 1 chitosan derivative is the preparation method of the MRI contrast agent of carrier, see Figure 1a , the specific steps are as follows: In an implementation case, the preparation method of the contrast agent may include the following steps:

[0034] (1) Dissolve PEG-COOH into a 5% (w / w) solution, then adjust the pH of the solution to 6, then add NHS, stir for 5 minutes and then add EDC to make the molar ratio of EDC:NHS:COO 1: 1:0.8. Stir the above solution for 30 minutes to activate the carboxyl group and slowly add it to the solution dissolved in 1% CH 3 In chitosan in COOH, the reaction solution was stirred at room temperature for 10 h. The reaction solution was dialyzed and then freeze-dried to obtain polyethylene glycol-modified chitosan (CS-PEG).

[0035] (2) Dissolving CS-PEG in an equal volume mixture of 5 wt% glacial acetic acid and hydrochloric acid, and adding azide epichlorohydrin. The reaction solution was protected from light with aluminum ...

Embodiment 2

[0039] Example 2 measures the infrared spectrograms of CS, CS-PEG, CS-PEG-N3 and CS-PEG-G2-DTPA-Gd, including: adopting the tablet method to prepare samples, and detecting chitosan raw materials, CS-PEG, CS respectively -Infrared absorption of PEG-N3 and CS-PEG-G2-DTPA-Gd, as figure 2 shown.

Embodiment 3

[0040] Example 3 Test the polymer contrast agent of the present invention and the relaxation time T of Gd-DTPA on a 0.5T MRI tester1 and T 1 Weighted imaging, including:

[0041] Prepare the above two samples with a concentration of 0.1 to 1.0 mM respectively. After the test, use the concentration as the abscissa and the reciprocal of the relaxation time as the ordinate to perform linear fitting to obtain the relaxation rates of the contrast agent of the present invention and Gd-DTPA, respectively. 9.53mM -1 ·s -1 and 4.25mM -1 ·s -1 ( image 3 ). The relaxation rate of the contrast agent of the present invention is obviously higher than that of Gd-DPTA. Through the T of both at different concentrations 1 weighted imaging ( Figure 4 ) It can be seen that both of them tend to become brighter with the increase of the concentration, but the contrast effect of the contrast agent of the present invention is obviously brighter than that of Gd-DTPA.

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Abstract

The invention discloses an MRI contrast agent taking a chitosan derivative as a carrier and a preparation method of the contrast agent. The contrast agent comprises chitosan which serves as a main body of the contrast agent and modified with polyethylene glycol and a secondary polyamide dendrimer which is mainly connected to a main chain of chitosan and provided with a gadolinium chelate. The preparation method of the contrast agent comprises the steps that chitosan modified with polyethylene glycol is provided, a chelating ligand of gadolinium is coupled to the secondary polyamide dendrimer modified with an alkynyl group, then the modified secondary polyamide dendrimer is connected to chitosan, and the contrast agent is obtained. The MRI contrast agent taking the chitosan derivative as the carrier is good in biocompatibility, easy to biologically degrade and high in relaxation rate, the preparation method is simple, the needed reaction temperature is moderate, and control is easy.

Description

technical field [0001] The invention relates to a contrast agent for magnetic resonance imaging, in particular to a chitosan-based MRI contrast agent for magnetic resonance imaging contrast and a preparation method thereof, belonging to the technical field of medical clinical magnetic resonance imaging. Background technique [0002] With the development of science and technology, magnetic resonance imaging has become an effective means of clinical detection of solid tumors. Compared with other imaging techniques, magnetic resonance imaging has many advantages, such as no ionizing radiation damage, ultra-high tissue resolution and three-dimensional positioning ability. However, in order to further improve the sensitivity and accuracy of imaging, contrast agents are usually required to enhance the imaging contrast. At present, the clinical contrast agent is generally a small molecule gadolinium chelate. There are still some disadvantages in the application of this type of sm...

Claims

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Application Information

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IPC IPC(8): A61K49/12
Inventor 裴仁军仝晓艳刘敏
Owner SUZHOU INST OF NANO TECH & NANO BIONICS CHINESE ACEDEMY OF SCI
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