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Graphene oxide nano-drug carrier and anti-tumor drug as well as preparation method of anti-tumor drug

A nano-drug carrier and anti-tumor drug technology, applied in anti-tumor drugs, drug combinations, pharmaceutical formulations, etc., can solve the problems of poor stability, easy agglomeration, and metabolism of graphene oxide

Active Publication Date: 2013-09-25
SHENZHEN INST OF ADVANCED TECH CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, graphene oxide as a drug carrier also has its own defects. The stability of unmodified graphene oxide in the human body is very poor, and it is prone to agglomeration and cannot be completely metabolized by organisms.

Method used

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  • Graphene oxide nano-drug carrier and anti-tumor drug as well as preparation method of anti-tumor drug
  • Graphene oxide nano-drug carrier and anti-tumor drug as well as preparation method of anti-tumor drug
  • Graphene oxide nano-drug carrier and anti-tumor drug as well as preparation method of anti-tumor drug

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Experimental program
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preparation example Construction

[0042] The preparation method of antitumor drug of one embodiment, comprises the steps:

[0043] Adding graphene oxide, pyrenyl dithiopolyethylene glycol and hydrophobic drugs with anti-tumor efficacy into water to obtain a mixture, the mixture was ultrasonically treated at room temperature for 2 hours, filtered and freeze-dried to obtain anti-tumor drugs.

[0044] Among them, the anti-tumor drugs include graphene oxide nanometer drug carriers and hydrophobic drugs with anti-tumor efficacy. The graphene oxide nano-medicine carrier includes a plurality of nanoparticles, and each nanoparticle includes an inner core formed by graphene oxide and an outer shell formed by adhering pyrenyl disulfide polyethylene glycol to the surface of the inner core. Wherein, pyrenyl dithiopolyethylene glycol adheres to the surface of graphene oxide through the π-π conjugation effect of pyrenyl and graphene oxide to form a shell. Hydrophobic drugs with anti-tumor efficacy are loaded on the inner c...

Embodiment 1

[0060] Weigh 0.17g of cystamine hydrochloride (1.1mmol) and 88mg of NaOH (2.2mmol) into 30mL of water, stir at room temperature for 30min, and then remove water by vacuum rotary evaporation at 45°C. Dichloromethane was added to the above mixture, the precipitate was filtered, and the dichloromethane was removed by vacuum rotary evaporation at 30°C. A pale yellow liquid cystamine was obtained. Take 120mg EDC·HCl (0.62mmol), 28mg NHS (0.23mmol), 1g mPEG-COOH (weight average molecular weight 5000) and 30mL dichloromethane at room temperature N 2 After reacting in the atmosphere for 5 hours, slowly drop 0.15 g of cystamine, and then react at room temperature for 24 hours to obtain a compound (mPEG-S-S-NH 2 );

[0061] Pipette 288 mg of pyrenebutyric acid, 287 mg of EDC·HCl, and 178 mg of NHS in 20 mL of dichloromethane for 2 h at room temperature, then add 0.5 g of mPEG-S-S-NH 2 Afterwards, after reacting at room temperature for 24h, obtain pyrenyl disulfide polyethylene glycol...

Embodiment 2

[0065] Weigh 0.17g of cystamine hydrochloride (1.1mmol) and 88mg of NaOH (2.2mmol) into 30ml of water, stir at room temperature for 30min, and then remove water by vacuum rotary evaporation at 45°C. Dichloromethane was added to the above mixture, the precipitate was filtered, and the dichloromethane was removed by vacuum rotary evaporation at 30°C. A pale yellow liquid cystamine was obtained. Take 120mg EDC·HCl (0.62mmol), 28mg NHS (0.23mmol), 1gmPEG-COOH (weight average molecular weight 5000), 30ml dichloromethane at room temperature 2 After reacting in the atmosphere for 5 hours, slowly drop 0.15g cystamine and react at room temperature for 24 hours to obtain mPEG-S-S-NH 2

[0066] Pipette 288mg pyrenebutyric acid, 287mgEDC·HCl, 178mgNHS in 20ml dichloromethane and activate at room temperature for 2h, then add 0.5gmPEG-S-S-NH 2 Finally, after reacting at room temperature for 24 hours, pyrene-S-S-PEG was obtained.

[0067] Pipette 2mg of graphene oxide, 10mg of pyrene-S-S...

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Abstract

The invention relates to a graphene oxide drug carrier and an anti-tumor drug as well as a preparation method of the anti-tumor drug. The graphene oxide drug carrier comprises multiple nano-particles, wherein each nano-particle comprises an inner core formed by graphene oxide and a shell formed by pyrenyl disulfide group polyethylene glycol, and the pyrenyl disulfide group polyethylene glycol is adhered to the surface of the graphene oxide through the pi-pi conjugative effect of pyrenyl and the graphene oxide. The modification effect of the pyrenyl disulfide group polyethylene glycol ensures that the graphene oxide drug carrier has the characteristics of relatively high space stability, electrostatic stability and has relatively high stability.

Description

technical field [0001] The invention relates to the technical field of drug carriers, in particular to a graphene oxide drug carrier, an antitumor drug and a preparation method thereof. Background technique [0002] Graphene oxide has the characteristics of low toxicity and large surface energy, so it can be used as a drug carrier in the field of biomedicine. Graphene oxide as a drug carrier has incomparable advantages over other carriers, for example, photothermal therapy can be performed by utilizing the properties of graphene oxide itself. At the same time, the graphene oxide drug carrier is much larger than the general drug carrier, and its drug loading is also much larger than the former. However, graphene oxide as a drug carrier also has its own defects. Unmodified graphene oxide has poor stability in the human body, is prone to agglomeration, and cannot be completely metabolized by organisms. Contents of the invention [0003] Based on this, it is necessary to pro...

Claims

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Application Information

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IPC IPC(8): A61K47/34A61K47/04A61K45/00A61K31/704A61K31/4745A61K31/337C08G65/48A61P35/00A61K47/60A61K47/69
Inventor 蔡林涛邓吉喆刘斌
Owner SHENZHEN INST OF ADVANCED TECH CHINESE ACAD OF SCI
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