A chemical exchange saturation transfer contrast agent and its preparation method and application

A technology of chemical exchange and contrast agent, which is used in pharmaceutical formulations, preparations for in vivo testing, and emulsion delivery to achieve high safety, high sensitivity, and improve the effect of EPR.

Active Publication Date: 2021-11-09
HARBIN MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0011] However, due to the complex composition in the body, there are many interference factors to the magnetic field, such as the direct water saturation effect (directwater saturation, DS) and the conventional MT effect (conventional MT contrast, MTC) of the semi-solid pool, plus the NOE (Nuclear Overhauser Effect, NOE ) effect, the synthesis and discovery of CEST contrast agents with high efficiency, high sensitivity, high biocompatibility and high safety still bring certain technical challenges and difficulties

Method used

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  • A chemical exchange saturation transfer contrast agent and its preparation method and application
  • A chemical exchange saturation transfer contrast agent and its preparation method and application
  • A chemical exchange saturation transfer contrast agent and its preparation method and application

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preparation example Construction

[0057] Such as figure 1 As shown, another embodiment of the present invention provides a preparation method of a chemical exchange saturation transfer contrast agent. The method specifically may include the following steps:

[0058] Uniformly mix the iodine contrast agent with ultrapure water or PBS buffer to obtain the iodine contrast agent mixture. Wherein, the molar ratio of iodine contrast agent to ultrapure water is 8:1.

[0059] Dissolve the surfactant with chloroform or ether solvent.

[0060] Add the iodine contrast agent mixture to the dissolved surfactant, ultrasonicate for 10 minutes in an ice bath, remove the organic phase at room temperature, and dialyze to obtain a chemical exchange saturation transfer contrast agent made of surfactant-coated iodine contrast agent .

[0061] Further, the definitions of surfactant and iodine contrast agent are as above. For example, the surfactant is one or a mixture of phosphatidylcholine liposomes, phosphatidylethanolamine ...

Embodiment 1

[0070] Preparation of lipoCEST contrast agent

[0071] 1) uniformly mixing iohexol and ultrapure water to obtain iohexol mixed solution;

[0072] 2) dissolving lecithin and cholesterol with chloroform to obtain the dissolved surfactant, wherein lecithin:cholesterol=8:1 (molar ratio);

[0073] 3) Add the iohexol mixture to the dissolved surfactant (iohexol:surfactant = 1:1 (molar ratio)), use a probe-type ultrasonic ice bath to sonicate for 10 minutes, and use a rotary evaporator The organic phase was removed at room temperature, followed by dialysis to obtain lipoCEST nanoparticles, namely lipoCEST contrast agent.

[0074] figure 2 The DLS plot of the resulting lipoCEST nanoparticles is shown, as figure 1As shown, its particle size (hydrated particle size) is basically distributed in the range of 70-240nm (the particle size of 116nm accounts for about 97.4%), mainly concentrated around 100nm, which is in line with the size supported by the EPR effect.

[0075] image 3 A...

Embodiment 2

[0086] Preparation of lipoCEST contrast agent

[0087] 1) uniformly mixing iopamidol and ultrapure water to obtain iopamidol mixed solution;

[0088] 2) dissolving lecithin and cholesterol with chloroform to obtain the dissolved surfactant, wherein lecithin:cholesterol=8:1 (molar ratio);

[0089] 3) Add the iopamidol mixture to the dissolved surfactant (iopadol:surfactant = 1:0.8 (molar ratio)), ultrasonicate for 10 minutes with a probe-type ultrasonic ice bath, and use a rotary evaporator The organic phase was removed at room temperature, followed by dialysis to obtain lipoCEST nanoparticles, namely lipoCEST contrast agent.

[0090] The signal strength of CEST is shown in Table 1.

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Abstract

The disclosure provides a chemical exchange saturation transfer contrast agent and its preparation method and application, belonging to the technical field of nuclear magnetic resonance imaging. The contrast agent is a new type of LipoCEST contrast agent. On the basis of retaining the advantages of high sensitivity of the original iodine-based CEST contrast agent, it also has high biocompatibility and safety, and solves the problem of traditional CEST contrast agents such as iohexol. The disadvantages such as fast excretion in the tumor area and low retention rate improve the EPR effect in the tumor area. The contrast agent is formed by wrapping an iodine contrast agent with a surfactant, and the surfactant is selected from one or more of phosphatidylcholine liposomes, phosphatidylethanolamine liposomes, phosphatidylserine, lecithin or cholesterol. mixture of species. This contrast agent is used in magnetic resonance imaging.

Description

technical field [0001] The invention relates to the technical field of magnetic resonance imaging, in particular to a chemical exchange saturation transfer contrast agent and its preparation method and application. Background technique [0002] Magnetic resonance imaging (MRI, magnetic resonance imaging) is an advanced medical imaging diagnostic technology, which uses different resonance signals generated by different tissues of the body under external magnetic field imaging. The strength of the magnetic resonance signal depends on the water content and The relaxation time of protons in water molecules can effectively detect tissue necrosis, ischemia and respective malignant lesions, etc. [0003] In clinical MRI, contrast agent (contrast agent, contrast agent) is an imaging enhancement contrast agent used to shorten imaging time, improve imaging contrast and clarity, can change the relaxation rate of water protons in local tissues in the body, and improve normal Imaging co...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K49/18A61K49/10
CPCA61K49/10A61K49/1812
Inventor 孙夕林吴丽娜阿荣王凯杨丽丽程立欣
Owner HARBIN MEDICAL UNIVERSITY
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