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A kind of nano-medicine simulating superoxide dismutase/catalase, preparation method and application thereof

A catalase and nano-drug technology, applied in the application of oxidative stress-related diseases, in the field of composition of nano-drugs, can solve the problems of high cost, complex synthesis process of drugs or carrier materials, etc., to ensure safety, guarantee Feasibility and safety, the effect of efficient targeted enrichment

Active Publication Date: 2019-06-18
ARMY MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although many nano-drugs have been used in the prevention and treatment of IBD in research at home and abroad; however, they face high costs (especially peptide and nucleic acid drugs), complex synthesis processes of drugs or carrier materials, and complex preparation of nano-drugs in their clinical transformation. Process stability and nanomedicine treatment controllability and other issues

Method used

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  • A kind of nano-medicine simulating superoxide dismutase/catalase, preparation method and application thereof
  • A kind of nano-medicine simulating superoxide dismutase/catalase, preparation method and application thereof
  • A kind of nano-medicine simulating superoxide dismutase/catalase, preparation method and application thereof

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Experimental program
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Effect test

Embodiment 1

[0036] First, 1 mg of lecithin and 9 mg of polyethylene glycol-distearoyl phosphatidylethanolamine (polyvinyl alcohol with a molecular weight of 1000 Da) are dissolved in 10 mL of double-distilled water at a constant temperature of 65°C under magnetic stirring. When the solid matter is completely dissolved, Leave to cool to room temperature. 30 mg of 4-hydroxymethyl phenylboronic acid pinacol ester modified α-cyclodextrin derivative and 10 mg of 2,2,6,6-tetramethylpiperidine oxide were dissolved in 1.2 mL of methanol. Then, under stirring conditions, the organic phase was slowly added dropwise to the water phase (1 mL / min). After the dropwise addition is completed, continue stirring at 25°C for 2 hours to volatilize and remove the organic solvent. After centrifugal separation, washing with deionized water, and freeze-drying, the nano medicine of the present invention can be obtained.

Embodiment 2

[0038] First dissolve 4mg lecithin and 6mg polyethylene glycol-distearoylphosphatidylethanolamine (the molecular weight of polyvinyl alcohol is 2000Da) in 10mL double-distilled water under the condition of constant temperature magnetic stirring at 65℃. When the solid matter is completely dissolved, Leave to cool to room temperature. Dissolve 30 mg of 4-hydroxymethyl phenylboronic acid pinacol ester modified α-cyclodextrin derivative and 10 mg of 4-hydroxy-2,2,6,6-tetramethylpiperidine oxide in 1.2 mL methanol / In acetonitrile. Then, under stirring conditions, the organic phase was slowly added dropwise to the water phase (1 mL / min). After the addition is complete, continue stirring at 30°C for 4 hours to volatilize and remove the organic solvent. After centrifugal separation, washing with deionized water, and freeze-drying, the nano medicine of the present invention can be obtained.

Embodiment 3

[0040] First, 4mg lecithin and 6mg polyethylene glycol-distearoylphosphatidylethanolamine (polyvinyl alcohol has a molecular weight of 2000Da) are dissolved in 10mL double-distilled water at 65°C under constant magnetic stirring conditions. When the solid matter is completely dissolved, Leave to cool to room temperature. Dissolve 30 mg 4-hydroxymethyl phenylboronic acid pinacol ester modified β-cyclodextrin derivative and 10 mg 4-amino-2,2,6,6-tetramethylpiperidine oxide in 1.2 mL methanol / In dimethylformamide. Then, under stirring conditions, the organic phase was slowly added dropwise to the water phase (1 mL / min). After the addition is completed, continue stirring at 60°C for 8 hours to volatilize and remove the organic solvent. After centrifugal separation, washing with deionized water, and freeze-drying, the nano medicine of the present invention can be obtained.

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Abstract

The invention relates to a nano-drug simulating superoxide dismutase or catalase and a preparation method and application thereof. A nano-carrier is prepared from cyclodextrin derivatives with the hydrogen peroxide removing capacity, free radical scavenger drugs, lecithin and polyethylene glycol-distearoyl-phosphatidylethanolamine, wherein the mass ratio of the polyethylene glycol-distearoyl-phosphatidylethanolamine to the cyclodextrin derivatives is 2:100-1:1. The nano-drug prepared through the method is in a spherical shape, the particle size range is about 20-800 nm, and the free radical scavenger drugs are evenly distributed in the nano-drug. The preparation method comprises the steps that firstly, the lecithin and the polyethylene glycol-distearoyl-phosphatidylethanolamine are dissolved in water to obtain a water phase, and the cyclodextrin derivatives and the free radical scavenger drugs are dissolved in organic solvent to obtain an organic phase; secondly, the organic phase is slowly and dropwise added in the preheated water phase, centrifugal washing is performed, freeze drying is performed, and then the nano-drug is obtained. The nano-drug has the obvious preventing and treating effects on oxidative stress injury correlation diseases such as inflammatory bowel diseases, myocardial infarction and congestive heart failure.

Description

Technical field [0001] The invention relates to a nano-medicine for resisting oxidative stress damage, in particular to the composition and preparation of a nano-medicine that simulates superoxide dismutase / catalase, and its use in the prevention and treatment of inflammatory bowel disease and other oxidative stress-related diseases In the application. Background technique [0002] The occurrence, development and malignancy of many diseases are closely related to the production of abnormally high levels of reactive oxygen species (ROS), including inflammatory bowel disease (IBD), myocardial infarction, and heart failure. Inflammatory bowel disease (IBD) is a chronic inflammatory disease of the gastrointestinal tract. Clinically, it mainly includes Crohn's disease and non-specific ulcerative colitis, which seriously affect human health. Although the exact cause of IBD is still unclear, there is a lot of evidence that genetic factors, immune system, and environmental factors (incl...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K45/06A61K9/19A61K31/724A61K47/24A61P1/00A61P9/04A61P9/10A61P39/06A61K31/445
CPCA61K9/0053A61K9/19A61K31/445A61K31/724A61K45/06A61K47/24A61K2300/00
Inventor 张建祥张齐雄李晓辉张定林
Owner ARMY MEDICAL UNIV
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