Graphdiyne nano preparation, preparation method thereof and application of graphdiyne nano preparation in preparation of medicine for treating Parkinson's disease

A nano-preparation and graphyne technology, applied in the direction of nano-medicine, nano-carbon, drug combination, etc., can solve the problems of lack of treatment methods, achieve high drug loading capacity, improve brain delivery efficiency, and improve brain drug delivery efficiency. Effect

Pending Publication Date: 2021-08-10
GUANGZHOU UNIVERSITY OF CHINESE MEDICINE +1
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0002] Neurodegenerative diseases pose a huge threat to human health. Among them, Parkinson's disease is the second largest neurodegenerative disease. With the aging of the population, its incidence will further increase. However, there is currently a lack of Effective treatment, ur

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  • Graphdiyne nano preparation, preparation method thereof and application of graphdiyne nano preparation in preparation of medicine for treating Parkinson's disease
  • Graphdiyne nano preparation, preparation method thereof and application of graphdiyne nano preparation in preparation of medicine for treating Parkinson's disease
  • Graphdiyne nano preparation, preparation method thereof and application of graphdiyne nano preparation in preparation of medicine for treating Parkinson's disease

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Embodiment 1

[0059] An embodiment of the present invention, this embodiment provides a preparation method of GDY and PEG-GDY, the preparation method is:

[0060] (1) graphyne preparation:

[0061] 43.6 mg of hexa[(trimethylsilyl)ethynyl]benzene and 15 mL of tetrahydrofuran solution containing 0.4 mmol of tetrabutylammonium fluoride were stirred and reacted at 8°C for 10 min, then 10 mL of ethyl acetate was added, and the reaction product was washed with brine, And add 20g of anhydrous sodium sulfate to dry. Subsequently, the resulting product was dried at room temperature under vacuum until the solvent was completely evaporated, and dispersed in pyridine at a ratio of 25 mL of pyridine per 10 mg of the product, and the resulting solution was slowly added to a copper foil filled with nitrogen, and the reaction was stirred for 2 days. At this time, A graphdiyne film will appear on the surface of the copper foil. Subsequently, the copper foil was washed with 10 mL of acetone and 10 mL of di...

Embodiment 2

[0068] An embodiment of the present invention, this embodiment provides a photothermal behavior of PEG-GDY. Prepare PEG-GDY solutions with gradient concentrations (15.6 μg / mL, 31.3 μg / mL, 62.5 μg / mL, 125 μg / mL). Place the PEG-GDY solutions with gradient concentrations in transparent quartz dishes respectively, at 1W / cm 2 Intensity 808nm near-infrared light was irradiated for 5 minutes, and the temperature changes were recorded respectively. In addition, the light-to-heat conversion coefficient was about 32%. The calculation formula is as follows:

[0069] η=(hA△T max –Q) / I(1-10 -Aλ )

[0070] In the formula, η is the light-to-heat conversion efficiency, h is the heat transfer coefficient of dispersed light and heat, A is the surface area of ​​the container, and ΔT max is the maximum temperature rise under near-infrared light, I is light intensity, -A 808 is the absorbance of PEG-GDY under near-infrared light irradiation, and Q is the heat absorbed by the pure dispersion l...

Embodiment 3

[0073] An embodiment of the present invention, this embodiment provides a method for loading MN with PEG-GDY. First prepare different proportions of MN aqueous solutions (3.91 μg / mL, 7.81 μg / mL, 15.6 μg / mL, 31.3 μg / mL, 62.5 μg / mL), measure the absorbance at 365 nm with a UV-visible spectrophotometer, and draw the concentration-absorbance standard curve line. Take 1 mg of PEG-GDY aqueous solution with a concentration of 1 mg / mL at a concentration of 1 mg / mL, and add a concentration of 1 mg / mL according to the volume ratio of PEG-GDY aqueous solution and MN aqueous solution at 1:0.5, 1:1, 1:2, and 1:3, respectively. MN aqueous solution was stirred overnight, and centrifuged at 12000rpm for 5min to obtain MN-PEG-GDY, and the MN content in the supernatant was determined to calculate the drug loading rate and drug loading amount. Depend on image 3 As shown in B and 3C, the drug loading rate of MN decreases with the increase of the feed ratio, while the drug load increases with t...

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Abstract

The invention discloses a graphdiyne nano preparation, a preparation method thereof and an application of the graphdiyne nano preparation in preparation of a medicine for treating Parkinson's disease. The graphdiyne nano preparation comprises graphdiyne nanosheets of which the surfaces are modified with polyethylene glycol and dimethylamine tetracycline. The graphdiyne nanosheet has a relatively high specific surface area, and the surface is electronegative, so that medicine loading is easy to realize. Besides, the graphdiyne nanosheets have high photothermal conversion capacity and can generate heat under near-infrared illumination, so that the permeability of a blood-brain barrier is improved, the nano drug delivery system has light controlled release capacity, the brain delivery efficiency of the dimethylamine tetracycline with a neuroprotective effect can be improved, and the Parkinson's disease resisting curative effect of the dimethylamine tetracycline can be improved.

Description

technical field [0001] The invention belongs to the application field of medical materials, and in particular relates to a graphyne nano-preparation, a preparation method thereof, and an application in preparing a drug for treating Parkinson's disease. Background technique [0002] Neurodegenerative diseases pose a huge threat to human health. Among them, Parkinson's disease is the second largest neurodegenerative disease. With the aging of the population, its incidence will further increase. However, there is currently a lack of There is an urgent need to develop new anti-Parkinson's disease drugs for effective treatment. Due to the existence of the blood-brain barrier, it is difficult for drug molecules to smoothly enter the brain and reach the lesion area, which brings great challenges to the development of anti-Parkinson's disease drugs. [0003] The application of nanotechnology in the research and development of Parkinson's disease drugs is beneficial to increase the ...

Claims

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Application Information

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IPC IPC(8): A61K47/69A61K41/00A61K47/60A61K31/65A61P25/16B82Y5/00B82Y20/00B82Y30/00B82Y40/00C01B32/15
CPCA61K47/60A61K41/0052A61K31/65A61K47/6923A61K9/0019A61P25/16B82Y5/00B82Y20/00B82Y30/00B82Y40/00C01B32/15
Inventor 陈桐楷李田忠刘瑶谢中建张晗程国旺罗景山
Owner GUANGZHOU UNIVERSITY OF CHINESE MEDICINE
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