Nanoparticle loaded with near-infrared emission fluorescent molecule/sorafenib and preparation method of nanoparticle

A fluorescent molecule and nanoparticle technology, applied in the field of medicine and nanotechnology applications, can solve the problems of no effective means to monitor the efficacy of drugs, poor water solubility of sorafenib, and low bioavailability.

Pending Publication Date: 2021-08-31
SOUTH CHINA UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0005] In order to solve the problems of poor water solubility of Sorafenib, low bioavailability and no effective means to monitor the curative effect of the drug, the invention provides a nanoparticle loaded with near-infrared emit...

Method used

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  • Nanoparticle loaded with near-infrared emission fluorescent molecule/sorafenib and preparation method of nanoparticle
  • Nanoparticle loaded with near-infrared emission fluorescent molecule/sorafenib and preparation method of nanoparticle
  • Nanoparticle loaded with near-infrared emission fluorescent molecule/sorafenib and preparation method of nanoparticle

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Weigh 10 mg of polyoxyethylene polyoxypropylene ether block copolymer with a molecular weight of 5000, 1 mg of sorafenib toluenesulfonic acid, and 1 mg of pyrrolopyrrole azafluoroboron compound into 3 sample bottles, and then add 2 mL of tetrahydrofuran , fully stirred and dissolved to obtain solution A, solution B and solution C. Under continuous stirring, mix solutions A, B, and C evenly, add 20 mL of ultrapure water dropwise to the above mixed solution under ultrasonic conditions, and transfer the resulting solution to a dialysis bag with a molecular weight cut-off of Mw=3500Da for dialysis, every 3 Change the water once every hour, and perform dialysis for 48 hours. After the dialysis, filter through a 0.22 μm filter membrane to remove unloaded sorafenib and pyrrolopyrrole azafluoroboron compounds, and obtain loaded near-infrared emitting fluorescent molecules / Nanoparticles of Sorafenib. Perform dynamic light scattering, ultraviolet, and fluorescence emission ana...

Embodiment 2

[0021] Weigh 100 mg of polyoxyethylene polyoxypropylene ether block copolymer with a molecular weight of 9000, 10 mg of sorafenib toluenesulfonic acid, and 10 mg of pyrrolopyrrole azafluoroboron compound into 3 sample bottles, and then add 5 mL of tetrahydrofuran , fully stirred and dissolved to obtain solution A, solution B and solution C. Under continuous stirring, mix solutions A, B, and C evenly, add 50 mL of ultrapure water dropwise to the above mixed solution under ultrasonic conditions, and transfer the resulting solution to a dialysis bag with a molecular weight cut-off of Mw=3500Da for dialysis, every 3 Change the water once every hour, and perform dialysis for 48 hours. After the dialysis, filter through a 0.22 μm filter membrane to remove unloaded sorafenib and pyrrolopyrrole azafluoroboron compounds, and obtain loaded near-infrared emitting fluorescent molecules / Nanoparticles of Sorafenib.

Embodiment 3

[0023] Weigh 1000mg of polyoxyethylene polyoxypropylene ether block copolymer with a molecular weight of 4000, 10mg of sorafenib toluenesulfonic acid, and 10mg of pyrrolopyrrole azafluoroboron compound into 3 sample bottles, and then add 10mL of tetrahydrofuran , fully stirred and dissolved to obtain solution A, solution B and solution C. Under continuous stirring, mix solutions A, B, and C evenly, add 200 mL of ultrapure water dropwise to the above mixed solution under ultrasonic conditions, and transfer the resulting solution to a dialysis bag with a molecular weight cut-off of Mw=3500Da for dialysis, every 3 Change the water once every hour, and perform dialysis for 48 hours. After the dialysis, filter through a 0.22 μm filter membrane to remove unloaded sorafenib and pyrrolopyrrole azafluoroboron compounds, and obtain loaded near-infrared emitting fluorescent molecules / Nanoparticles of Sorafenib.

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Abstract

The invention discloses a nanoparticle loaded with near-infrared emission fluorescent molecules/sorafenib and a preparation method of the nanoparticle. The nanoparticle is prepared from a macromolecular wrapping agent polyoxyethylene polyoxypropylene ether segmented copolymer, a near-infrared emission fluorescent molecule pyrrolo-pyrrole aza-fluorine boron compound and sorafenib. The average hydrated particle size of the obtained nanoparticles is 90-150nm, so that the water solubility, stability and water dispersibility of sorafenib are improved, and a fluorescence monitoring means is provided for research on pharmacokinetics, drug distribution, drug metabolic pathways and the like of sorafenib. The preparation method comprises the following steps: respectively preparing the polyoxyethylene polyoxypropylene ether segmented copolymer, the pyrrolo-pyrrolo-aza-fluorine boron compound and the sorafenib salt into solutions, then mixing, adding deionized water, fully stirring, dialyzing, and carrying out membrane filtration to obtain the product.

Description

technical field [0001] The invention relates to the application fields of medicine and nanotechnology, in particular to nanoparticles loaded with near-infrared emitting fluorescent molecules / sorafenib. Background technique [0002] Sorafenib is an oral multi-target molecular targeting agent, which can prolong the life of patients with advanced cellular liver cancer. In 2007, the US Food and Drug Administration approved it as a first-line drug in the standard treatment of advanced liver cancer. Although Sorafenib has shown a good curative effect in clinical treatment, its toxic side effects and drug resistance cannot be ignored, including: (1) Sorafenib has poor water solubility, low bioavailability, and is susceptible to Dietary influence; (2) Sorafenib is very cytotoxic, and the drug molecules will be distributed throughout the body, resulting in a series of serious side effects, such as diarrhea, dysentery, weight loss, high blood pressure, anorexia, voice change, nausea ...

Claims

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Application Information

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IPC IPC(8): A61K9/51A61K31/44A61K47/34A61P35/00A61K49/00
CPCA61K9/5146A61K31/44A61P35/00A61K49/0021A61K49/0054A61K49/0093
Inventor 汪凌云陈镁换曹德榕
Owner SOUTH CHINA UNIV OF TECH
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