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A kind of preparation method of magnetic resonance imaging contrast agent of 19f-acunotate nanoemulsion

A magnetic resonance imaging and nanoemulsion technology, which is applied in the directions of preparations, pharmaceutical formulations, and emulsion delivery for in vivo experiments, can solve the problems of strong background signal interference and low sensitivity, and achieve good photodynamic therapy effect and high sensitivity. , good biocompatibility

Active Publication Date: 2021-07-23
WUHAN INST OF PHYSICS & MATHEMATICS CHINESE ACADEMY OF SCI
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

but traditional 1 H MRI has low sensitivity due to strong background signal interference in vivo

Method used

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  • A kind of preparation method of magnetic resonance imaging contrast agent of 19f-acunotate nanoemulsion
  • A kind of preparation method of magnetic resonance imaging contrast agent of 19f-acunotate nanoemulsion
  • A kind of preparation method of magnetic resonance imaging contrast agent of 19f-acunotate nanoemulsion

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0053] A sort of 19 The preparation method of the magnetic resonance imaging contrast agent of F-hole palm nanoemulsion comprises the steps:

[0054] (1) Preparation of nanoemulsion: 40mg phospholipid, 5mg Pluronic F-68, 3.1mg 19 F- Acupoint and 7.6mg 19 F-porphyrin was dissolved in 2 mL of a mixed organic solvent (chloroform / methanol=3 / 1), and the organic solvent was removed with a rotary evaporator at room temperature, so that the raw material formed a lipid film on the wall of the flask, and then vacuum-dried at 45 ° C for 30 min to make Remove the organic solvent, add 1mL ultrapure water to the flask to dissolve the film, then add 78mg of 1,1,1-tris(perfluoro-tert-butoxymethyl)ethane, use a sonicator to sonicate for 20min, and then The nanoemulsion was extruded three times with a 0.22 μm microporous membrane, and finally the nanoemulsion was obtained.

[0055] (2) 19 The preparation of F-acantara: under the conditions of anhydrous and nitrogen protection, add the N,N- ...

Embodiment 2

[0070] A sort of 19 The preparation method of the magnetic resonance imaging contrast agent of F-hole palm nanoemulsion comprises the steps:

[0071] (1) Preparation of nanoemulsion: 40mg phospholipid, 5mg Pluronic F-68, 3.1mg 19 F- Acupoint and 5.3mg 19 F-porphyrin was dissolved in 2 mL of a mixed solvent (chloroform / methanol=3 / 1), and the organic solvent was removed with a rotary evaporator at room temperature, so that the raw material formed a lipid film on the wall of the flask, and then vacuum-dried at 45 ° C for 1 hour. Remove the organic solvent, add 1mL ultrapure water to the flask to dissolve the film, then add 78mg of 1,1,1-tris(perfluoro-tert-butoxymethyl)ethane, use a sonicator to sonicate for 20min, and then The nanoemulsion was extruded 5 times with a 0.22 μm microporous membrane, and finally the nanoemulsion was obtained.

[0072] (2) 19 Preparation of F-Anaphyllum: Under the conditions of anhydrous and nitrogen protection, add the N,N- Dimethylformamide (D...

Embodiment 3

[0078] A sort of 19 The preparation method of the magnetic resonance imaging contrast agent of F-hole palm nanoemulsion comprises the steps:

[0079] (1) Preparation of nanoemulsion: 40mg phospholipid, 5mg Pluronic F-68, 3.1mg 19 F- Acupoint and 8.8mg 19 F-porphyrin was dissolved in 2 mL of a mixed solvent (chloroform / methanol=3 / 1), and the organic solvent was removed with a rotary evaporator at room temperature, so that the raw material formed a lipid film on the wall of the flask, and then vacuum-dried at 45 ° C for 1 hour. Remove the organic solvent, add 1mL ultrapure water to the flask to dissolve the film, then add 156mg of 1,1,1-tris(perfluoro-tert-butoxymethyl)ethane, use a sonicator to sonicate for 20min, and then The nanoemulsion was extruded three times with a 0.22 μm microporous membrane, and finally the nanoemulsion was obtained.

[0080] (2) 19 The preparation of F-acantara: under the conditions of anhydrous and nitrogen protection, add the N,N- Dimethylforma...

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Abstract

The invention discloses a 19 The preparation method of the magnetic resonance imaging imaging contrast agent of F-pointan microemulsion, the steps are: (1) the preparation of nanoemulsion: by phospholipid, Pluronic F-68, 19 F‑Point, 19 F-porphyrin and 1,1,1-tris(perfluoro-tert-butoxymethyl)ethane obtain nanoemulsion through ultrasonic emulsification; (2) 19 Preparation of F-Xuefan: Compound obtained by reacting with F-polyethylene glycol 19 F‑Xue Fan. (3) 19 Preparation of F-porphyrin: Reaction of porphyrin with F-polyethylene glycol to obtain compound 19 F‑Porphyrin. (4) Preparation of targeting molecules: Cholesterol-polyethylene glycol 2000-maleimide reacts with arginine-glycine-aspartic acid to obtain targeting molecules. (5) Preparation of targeted nanoemulsion: adding cholesterol-polyethylene glycol 2000-arginine-glycine-aspartic acid into the nanoemulsion, and shaking to obtain the targeted nanoemulsion. The method is simple and efficient, and the contrast agent has high sensitivity and good biocompatibility, can target lung cancer tumors for MR imaging and optical imaging, and is applied to early diagnosis and treatment of lung cancer.

Description

technical field [0001] The invention belongs to the technical field of nuclear magnetic resonance imaging, and more specifically relates to a 19 The preparation method of the magnetic resonance imaging contrast agent of the F-acuate nanoemulsion is applied to the targeted magnetic resonance imaging, optical imaging and photodynamic therapy of lung cancer tumors. Background technique [0002] In clinical disease diagnosis, nuclear magnetic resonance (NMR) has been widely used due to its advantages of no radiation, multiple functions, and high spatial and temporal resolution. but traditional 1 H MRI has low sensitivity due to strong background signal interference in the body. With the continuous development of magnetic resonance imaging technology, heteronuclear MRI (such as 31 P, 13 C, 19 F, 129 Xe) has been widely concerned and researched. [0003] As a new type of nanocarrier, nanoemulsion has the advantages of good biocompatibility, stability, and easy modification,...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K51/04A61K51/06A61K51/08A61K51/12A61P35/00A61K101/02A61K101/00
CPCA61K51/0485A61K51/0493A61K51/06A61K51/082A61K51/122A61P35/00
Inventor 周欣张怀彬陈世桢娄昕
Owner WUHAN INST OF PHYSICS & MATHEMATICS CHINESE ACADEMY OF SCI
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