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Disulfiram nano-particle, and preparation method and application thereof

A technology of nanoparticles and disulfiram, which is applied in the fields of nano-drug carriers and medicine, and achieves the effects of simple operation, low cost, and improved half-life

Active Publication Date: 2020-01-24
WENZHOU MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, metal nano oxide materials have certain biological toxicity, so how to modify their surface properties to improve biocompatibility is very important

Method used

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  • Disulfiram nano-particle, and preparation method and application thereof
  • Disulfiram nano-particle, and preparation method and application thereof
  • Disulfiram nano-particle, and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0030] The preparation of embodiment disulfiram nanoparticle

[0031] Reference example of preparation method

[0032] After silkworm cocoons are degummed with sodium bicarbonate weak alkali solution, they are completely dissolved with lithium bromide solution, and regenerated silk fibroin is obtained after dialysis with deionized water; 20 mg of disulfiram is dissolved in 2 mL of absolute ethanol to obtain 10 mg / mL of Lun solution, this solution was added to 6mL nano-zinc oxide suspension, after continuous stirring for 6 hours, slowly drop into 2mL silk fibroin aqueous solution and continue stirring for 6 hours, the resulting mixed solution was added to 30mL acetonitrile solution, mixed and stirred After 1 hour, the organic solvent was removed by rotary evaporation, and freeze-dried to obtain disulfiram nanoparticles.

[0033] According to the same method, the material ratio was changed to obtain the disulfiram nanoparticles of the following examples 1-12, and the ratio cont...

Embodiment 4

[0048] In vivo anti-tumor effect of embodiment 4 disulfiram nanoparticles

[0049] 4.1 Establishment of tumor-bearing mouse model

[0050] Press 2×10 6 For each cell, the logarithmic phase paclitaxel-resistant cells (MCF-7 / PTX) were inoculated in the axilla of female BABL / c nude mice weighing 18-20 g and aged 5-6 weeks. Observe and measure, when the transplanted tumor grows to 50-100mm 3 Then start random grouping. On the 2nd, 4th, and 6th days after grouping, each disulfiram preparation (10 mg / kg) was injected intravenously. Two weeks after the end of administration, the experiment was stopped, the mice were killed by cervical dislocation and weighed, the tumor was stripped and weighed, and the tumor inhibition rate was calculated: tumor inhibition rate%=[1-(average tumor weight of the administration group / average tumor weight of the negative group) Weight)] × 100%. .

[0051] 4.2 Experimental grouping

[0052] The experimental groups followed the normal saline group, ...

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Abstract

The invention discloses a disulfiram nano-particle, and a preparation method and application thereof. The nano-particle consists of disulfiram, nanometer metallic oxides and silk fibroins, and belongsto the technical field of nanometer drug carriers. The invention also discloses a preparation method for the nano-particle. The preparation method comprises the following steps of: firstly, slowly dripping disulfiram solutions into a nanometer metallic oxide dispersion liquid; continuously stirring, then, adding a silk fibroin solution to be continuously stirred, and finally, adding three times of acetonitrile for crosslinking solidification; and carrying out rotary evaporation to remove organic solvents, and carrying out freeze-drying to obtain the disulfiram nano-particle. The disulfiram nano-particle prepared by the preparation method is simple in preparation, is high in drug carrying amounts, is high in stability, can effectively inhibit the proliferation of tumor cells under a low dosage, and has a wide clinic application prospect, and the anti-tumor effect of the disulfiram nano-particle is obviously superior to a disulfiram drug.

Description

technical field [0001] The invention belongs to the technical field of nano-medicine carrier and medicine, in particular to a disulfiram nano-particle and its preparation method and its application in the preparation of anti-tumor therapeutic drugs. Background technique [0002] Disulfiram (DSF) is an anti-alcoholism drug approved by the FDA, and it is currently the most widely used traditional alcohol withdrawal drug. It can inhibit the oxidative metabolism of acetaldehyde by acetaldehyde dehydrogenase, and make the alcohol metabolite acetaldehyde accumulate in the body, so as to achieve the purpose of alcohol abstinence. DSF has good safety and no obvious side effects. In recent years, researchers have discovered that DSF has shown great potential in tumor research and treatment, and can kill a variety of tumor cells including breast cancer, rectal cancer, melanoma, and glioma in vivo and in vitro. Compared with traditional chemotherapeutic drugs, DSF has low toxicity, l...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/69A61K31/145A61K33/34A61K33/30A61K47/64A61P35/00B82Y5/00B82Y40/00
CPCA61K31/145B82Y5/00B82Y40/00A61K33/30A61K33/34A61K47/64A61K47/6923A61P35/00A61K2300/00Y02A50/30
Inventor 姚情寇龙发赵应征林蒙婷鲁翠涛徐荷林张元元杨洋
Owner WENZHOU MEDICAL UNIV
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