Tumor-targeted nuclear magnetic resonance/fluorescence dual-mode imaging contrast agent, preparation and applications thereof

A dual-mode imaging and nuclear magnetic resonance technology, which is applied in preparations for in vivo experiments, emulsion delivery, drug delivery, etc., can solve the problems of lack of tumor targeting and easy aggregation of probes, and achieve enhanced MRI signal intensity and near-infrared fluorescence signal intensity, high quantum yield, and low toxic and side effects

Active Publication Date: 2017-02-15
DALIAN INST OF CHEM PHYSICS CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, the probe has a hydrated particle size of 32nm, i

Method used

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  • Tumor-targeted nuclear magnetic resonance/fluorescence dual-mode imaging contrast agent, preparation and applications thereof
  • Tumor-targeted nuclear magnetic resonance/fluorescence dual-mode imaging contrast agent, preparation and applications thereof
  • Tumor-targeted nuclear magnetic resonance/fluorescence dual-mode imaging contrast agent, preparation and applications thereof

Examples

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Embodiment 1

[0057] Preparation of tumor-targeted nuclear magnetic resonance and near-infrared fluorescence dual-mode imaging contrast agent:

[0058] (1) Preparation of NMR amphiphile: Take 1.0026g of tri-tert-butyl 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) and dissolve it in dichloromethane (DCM), and 0.2448g N-hydroxysuccinimide (NHS) under the action of 1.8087g dicyclohexylcarbodiimide (DCC), activated at room temperature for 2h, then added 0.5065g hexadecylamine, stirred at room temperature for 12h , after suction filtration, the reaction product was precipitated with a large amount of ether, and vacuum-dried to obtain a milky white powder; then added to a mixture of trifluoroacetic acid (TFA) and DCM, stirred and reacted for 2 hours, the reaction solvent was removed by rotary evaporation, and the reaction product was washed with petroleum ether. Vacuum-dried to obtain a white oil; redissolve the white oil in water, add 0.3481 g of gadolinium acetate hydrate at t...

Embodiment 2

[0063] Preparation of tumor-targeted nuclear magnetic resonance and near-infrared fluorescence dual-mode imaging contrast agent:

[0064] (1) Preparation of NMR amphiphile: Take 1.0026g of tri-tert-butyl 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) and dissolve it in dichloromethane (DCM), and 0.2448g N-hydroxysuccinimide (NHS) under the action of 1.8087g dicyclohexylcarbodiimide (DCC), activate at room temperature for 2h, then add 0.5660g carbooctadecylamine, stir at room temperature Reaction for 12 hours, after suction filtration, precipitate the reaction product with a large amount of ether, and dry it in vacuum; then add it to the mixture of trifluoroacetic acid (TFA) and DCM, stir and react for 2 hours, remove the reaction solvent by rotary evaporation, wash the reaction product with petroleum ether, vacuum Dry to obtain a white oil; redissolve the white oil in water, add gadolinium acetate hydrate at the same time, adjust the pH of the solution to 5-6,...

Embodiment 3

[0069] Preparation of tumor-targeted nuclear magnetic resonance and near-infrared fluorescence dual-mode imaging contrast agent:

[0070](1) Preparation of NMR amphiphile: Take 1.0026g of tri-tert-butyl 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) and dissolve it in dichloromethane (DCM), and 0.2448g N-hydroxysuccinimide (NHS) under the effect of 1.8087g dicyclohexylcarbodiimide (DCC) activated at room temperature for 2h, then added 1.571g phospholipids, stirred at room temperature for 12h, pumped After filtration, the reaction product was precipitated with a large amount of diethyl ether, dried in vacuo; then added to a mixture of trifluoroacetic acid (TFA) and DCM, stirred for 2 hours, and the reaction solvent was removed by rotary evaporation, the reaction product was washed with petroleum ether, and dried in vacuo to obtain a white oil matter; redissolve the white oil in water, add gadolinium acetate hydrate at the same time, adjust the pH of the solutio...

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Abstract

The present invention provides a tumor-targeted nuclear magnetic resonance/fluorescence dual-mode imaging contrast agent, preparation and applications thereof. According to the present invention, the contrast agent is nanometer micro-particles formed by self-assembling a nuclear magnetic resonance amphiphilic molecule, a near-infrared fluorescent dye amphiphilic molecule and a tumor targeting amphiphilic molecule in a solution, can stably exists under a physiological pH value condition, can be specifically accumulated at a tumor site in a targeting manner, can significantly enhance the intensity of the MRI signal and the near-infrared fluorescence signal at a tumor lesion site, can improve the specificity and the sensitivity of nuclear magnetic resonance imaging and near infrared fluorescence imaging scanning, and is expected to be adopted as the contrast agent for fluorescence guidance during tumor resection surgeries and postoperative nuclear magnetic resonance monitoring.

Description

technical field [0001] The invention relates to a contrast agent for imaging diagnosis, in particular to a tumor-targeting nuclear magnetic resonance / fluorescence dual-mode imaging contrast agent, a preparation method thereof, and an application in nuclear magnetic resonance imaging and near-infrared fluorescence imaging. Background technique [0002] In the early stage of cancer, if the physiological and morphological changes of diseased organs or tissues can be detected quickly and accurately, and corresponding imaging information can be given, it is of great significance for the early diagnosis of cancer. Contrast agents are such substances that are injected into specific tissues or organs of the human body to produce density or other differences from normal tissue parts and visualize these differences, thereby providing important clinical information about diseases. [0003] MRI (Magnetic Resonance imaging, MRI) is a technology that utilizes the hydrogen nuclei of water ...

Claims

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Application Information

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IPC IPC(8): A61K49/10A61K49/18A61K49/00
Inventor 王辉辉谭明乾马小军吕国军
Owner DALIAN INST OF CHEM PHYSICS CHINESE ACAD OF SCI
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