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Amphiphilic graphene-gold thermal radiotherapy nano drug as well as preparation method and application thereof

A nano-drug and amphiphilic technology, which is applied in the field of amphiphilic graphene-gold thermal radiotherapy nano-drugs and its preparation, can solve the problems of sharp dose peak, killing local tumors, and inability to kill tumors, achieving increased uniformity and prolonged Cycle time, the effect of enhancing the thermal killing effect

Active Publication Date: 2017-10-24
CHANGZHOU NO 2 PEOPLES HOSPITAL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Proton / neutron therapy will form a sharp dose peak at the end of the range to kill the tumor, but there is a problem that the dose peak is too sharp, it will only kill local tumors, and it cannot evenly treat large-area tumors. Therefore, the broadening of the Bragg peak is an urgent problem to be solved at present

Method used

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  • Amphiphilic graphene-gold thermal radiotherapy nano drug as well as preparation method and application thereof
  • Amphiphilic graphene-gold thermal radiotherapy nano drug as well as preparation method and application thereof
  • Amphiphilic graphene-gold thermal radiotherapy nano drug as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Mix 10g of hexamethylene diisocyanate (sufficient excess) with 1g of graphene oxide in anhydrous N, N-dimethylformamide (DMF), and react at 80 degrees for 12h, the end of hexamethylene diisocyanate The isocyanate reacts with the carboxyl or hydroxyl groups on the surface of graphene oxide to connect to the surface of graphene oxide, and the product is washed several times with anhydrous DMF to remove unreacted diisocyanate. Then add 5-10g polyacrylic acid (molecular weight: 5000g / mol) to the reaction solution, react at 80 degrees for 12h, make the carboxyl group in the polyacrylic acid react with the isocyanate group at the other end of the diisocyanate, and obtain amphiphilic reduced graphene oxide (Amphophilic Graphene).

[0042] Load gold nanoparticles on the surface of amphiphilic graphene by in-situ growth method: 10 mg of amphiphilic graphene is ultrasonically dispersed in a water bath ultrasonic instrument for 30 min to make it uniformly dispersed; add 9 mL of 10...

Embodiment 2

[0047] The preparation method of amphiphilic graphene-gold thermoradiation therapy nano-medicine of the present invention is as follows:

[0048] Mix 100g of hexamethylene diisocyanate and 1g of graphene oxide in DMSO solvent, react at 80 degrees for 24 hours, the isocyanate at one end of hexamethylene diisocyanate reacts with the carboxyl or hydroxyl group on the surface of graphene oxide, and connects to the surface of graphene oxide. Then add 5g polyacrylic acid (molecular weight 2000g / mol) and 5g polyacrylic acid-polyethylene glycol monomethyl ether copolymer in reaction solution, wherein the molecular weight of polyacrylic acid is 5000g / mol, the molecular weight of polyethylene glycol monomethyl ether is 500-1000g / mol, under the condition of 80 for 24h, the carboxyl group in the polymer reacts with the isocyanate group at the other end of the diisocyanate to obtain amphiphilic graphene.

[0049] Load gold nanoparticles on the surface of amphiphilic graphene by seed-media...

Embodiment 3

[0054] The amphiphilic graphene (10mg) prepared in Example 1 was ultrasonically dispersed in a water-bath ultrasonic instrument for 30min to make it uniformly dispersed; 9mL of 100mM CTAB, 1000uL of 10mM HAuCl were added thereto 4 1000 μL of 100 mM ascorbic acid (AA), soaking the amphiphilic graphene in it for 1 min to generate amphiphilic graphene-gold nanoparticles, wherein the gold particles are dot-shaped.

[0055] Add 0.01mg membrane-penetrating peptide Tat to 2mg amphiphilic graphene-gold nanoparticles, under the action of coupling agent EDC (2mg) and NHS (2mg), the amino group on the surface of membrane-penetrating peptide Tat and the surface of amphiphilic graphene Carboxyl reaction to obtain amphiphilic graphene-gold thermal radiotherapy nanomedicine. In the amphiphilic graphene-gold thermal radiotherapy nanomedicine, the mass fraction of the amphiphilic graphene is 99.89%, and the mass fraction of the nano-gold particles is 0.1%. The mass fraction of tumor targeting...

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Abstract

The invention relates to an amphiphilic graphene-gold thermal radiotherapy nano drug which comprises amphiphilic graphene, nano gold particles loaded on the surface of amphiphilic graphene, and tumor targeted molecules connected on amphiphilic graphene. The invention also provides a preparation method of the amphiphilic graphene-gold thermal radiotherapy nano drug, which comprises the following steps: modified diisocyanate on the surface of graphene oxide, and then adding a polymer containing carboxyl to enable carboxyl to react with diisocyanate, so as to obtain amphiphilic graphene; carrying out in-situ growth of gold nano particles on the surface of amphiphilic graphene; and finally, adding tumor targeted molecules containing amino groups and coupling agents into the product to enable the tumor targeted molecules containing amino groups to react with carboxyl of amphiphilic graphene, so as to obtain the amphiphilic graphene-gold thermal radiotherapy nano drug. The invention also provides the application of the amphiphilic graphene-gold thermal radiotherapy nano drug serving as an anti-tumor drug. The prepared nano drug can be compounded with protons / neutrons for treating through thermal therapy and has a relatively strong killing effect on tumor cells.

Description

technical field [0001] The invention relates to the field of nanomaterial medicines, in particular to an amphiphilic graphene-gold thermal radiotherapy nanomedicine and its preparation method and application. Background technique [0002] Nanotechnology is an emerging science and technology with great market application potential, which has attracted the attention of many research fields. As a new type of material, nanomaterials have special properties that ordinary macroscopic materials do not have, bringing new research vitality to the fields of medicine, biology, materials, and physics. [0003] Graphene is a single-layer planar carbon nanomaterial with good electrical and thermal conductivity. In recent years, it has made great research progress in the fields of medicine and biology. Graphene oxide is the oxide of graphene, with a variety of oxygen-containing functional groups, such as carbonyl, carboxyl, hydroxyl and epoxy groups, etc., can obtain specific physical and...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K41/00A61K47/58A61K47/60A61K47/64A61P35/00
CPCA61K41/0042A61K41/0052A61K41/009
Inventor 罗居东徐英蒋华倪昕晔朱文宇孙志强焦旸张琦
Owner CHANGZHOU NO 2 PEOPLES HOSPITAL
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