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Compound, water-soluble hematoporphyrin nano-particles and preparation method and application of water-soluble hematoporphyrin nano-particles

A nanoparticle, water-soluble technology, applied in drug delivery, pharmaceutical formulations, preparations for in vivo tests, etc., can solve problems such as potential safety hazards and poor stability of gadolinium-containing contrast agents, achieve tight binding, shorten relaxation time, The effect of avoiding toxic hazards

Pending Publication Date: 2022-07-01
WUHAN UNITED IMAGING LIFE SCI INSTR CO LTD
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Problems solved by technology

[0004] The purpose of the present invention is to provide a compound, water-soluble hematoporphyrin nanoparticles and its preparation method and application, which are used to solve the problem of poor stability of gadolinium-containing contrast agents and potential safety hazards in the prior art

Method used

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  • Compound, water-soluble hematoporphyrin nano-particles and preparation method and application of water-soluble hematoporphyrin nano-particles

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preparation example Construction

[0029] For the third solution provided by the present invention, a preparation method of water-soluble hematoporphyrin nanoparticles is proposed. The method utilizes azobisisobutyronitrile as a free radical initiator to polymerize the double bond of heme with 2-methacrylic acid, thereby preparing the water-soluble hematoporphyrin nanoparticles in the second solution. Specifically include:

[0030] (1) adding hemin, 2-methacrylic acid and an initiator into a solvent, and ultrasonically dissolving to obtain a mixed solution. In this step, the mass ratio of hemin, 2-methacrylic acid and the initiator is (50~80):(3000~3500):(10~15), preferably, hemin, 2-methyl The mass ratio of acrylic acid and initiator is 65:3250:12.5, and the mixture is obtained by ultrasonic for 0.5 to 1 h. After ultrasonication, hemin is fully dissolved, which is conducive to the subsequent polymerization reaction; the initiator is preferably azobisisobutyronitrile. , any one or more of azobisisoheptanenitr...

Embodiment 1

[0037] The steps of preparing water-soluble hematoporphyrin nanoparticles in this embodiment are as follows:

[0038] (1) Dissolve 65 mg of heme, 3.25 g of 2-methacrylic acid, and 12.5 mg of azobisisobutyronitrile in 10 mL of deionized water and 10 mL of dimethylformamide, and ultrasonicate for 0.5 h to fully dissolve the heme to obtain mixture.

[0039] (2) Repeatedly replacing the above mixed solution with 5N high-purity nitrogen gas three times, maintaining nitrogen protection after degassing, heating and stirring at 80° C. for 24 hours to obtain a reaction solution.

[0040] (3) the above-mentioned reaction solution is cooled to room temperature, and the protective environment of the inert gas is removed, and 100 mL of deionized water is added to the reaction solution after the cooling to carry out quenching reaction; then the reaction solution after the quenching reaction is moved into 3000KD interception In a dialysis bag of molecular weight, dialysis was performed with...

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Abstract

The invention discloses a compound, a water-soluble hematoporphyrin nano-particle and a preparation method and application thereof.The water-soluble hematoporphyrin nano-particle is prepared through a reaction of hemin and 2-methacrylic acid, the hemin is a complex formed by chlorination of ferric ions and protoporphyrin, the T1 longitudinal relaxation time of water protons can be greatly shortened, and the water-soluble hematoporphyrin nano-particle can be used for preparing the water-soluble hematoporphyrin nano-particle. The contrast enhancement effect is shown, so that the contrast agent can be used as a contrast agent; meanwhile, ferric ions are tightly combined with protoporphyrin and are not easy to dissociate, so that the problem of toxic hidden danger of a contrast agent is effectively avoided.

Description

technical field [0001] The invention relates to the technical field of nuclear magnetic resonance imaging, in particular to a compound, a water-soluble hematoporphyrin nanoparticle and a preparation method and application thereof. Background technique [0002] Nuclear magnetic resonance is a physical phenomenon. As an analytical method, it is widely used in physics, chemical biology and other fields, and is often used in medical clinical testing. Magnetic resonance imaging (MRI) is quite different from radiation imaging in nuclear medicine. MRI mainly applies a radio frequency pulse of a certain frequency to the human body in a static magnetic field to excite the hydrogen protons in the human body. Magnetic resonance phenomenon; after stopping the pulse, protons generate MR signals during the relaxation process, and the detection of human tissue is completed through the processing of MR signal reception, spatial encoding and image reconstruction. [0003] Because of its hig...

Claims

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Application Information

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IPC IPC(8): C08F220/06C08F226/06A61K49/12A61K49/18
CPCC08F220/06A61K49/122A61K49/1818C08F226/06
Inventor 张肖肖彭程远
Owner WUHAN UNITED IMAGING LIFE SCI INSTR CO LTD
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