Nano-drug simulating superoxide dismutase or catalase and preparation method and application thereof

A catalase and nano-drug technology, applied in the application of oxidative stress-related diseases, in the field of nano-drug composition, can solve the problems of complex synthesis process and high cost of drugs or carrier materials, and ensure feasibility and safety. Safety, Guaranteed Safety, Ease of Removal

Active Publication Date: 2016-02-17
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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  • Nano-drug simulating superoxide dismutase or catalase and preparation method and application thereof
  • Nano-drug simulating superoxide dismutase or catalase and preparation method and application thereof
  • Nano-drug simulating superoxide dismutase or catalase and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036]First, 1 mg of lecithin and 9 mg of polyethylene glycol-distearoyl phosphatidyl ethanolamine (wherein the molecular weight of polyvinyl alcohol is 1000 Da) was dissolved in 10 mL of double-distilled water under the condition of constant temperature magnetic stirring at 65 ° C, until the solid matter was completely dissolved, Let cool to room temperature. 30 mg of 4-hydroxymethylphenylboronic 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. The organic phase was then slowly added dropwise to the aqueous phase (1 mL / min) with stirring. After the dropwise addition was completed, stirring was continued at 25° C. for 2 h to volatilize and remove the organic solvent. The nanomedicine of the present invention can be obtained after centrifugal separation, washing with deionized water, and freeze-drying.

Embodiment 2

[0038] First, 4 mg of lecithin and 6 mg of polyethylene glycol-distearoyl phosphatidyl ethanolamine (wherein the molecular weight of polyvinyl alcohol is 2000 Da) was dissolved in 10 mL of double distilled water under the condition of constant temperature magnetic stirring at 65 ° C, until the solid matter was completely dissolved, Let cool to room temperature. 30 mg of 4-hydroxymethylbenzeneboronic acid pinacol ester modified α-cyclodextrin derivative and 10 mg of 4-hydroxy-2,2,6,6-tetramethylpiperidine oxide were dissolved in 1.2mL methanol / in acetonitrile. The organic phase was then slowly added dropwise to the aqueous phase (1 mL / min) with stirring. After the dropwise addition was completed, stirring was continued at 30° C. for 4 h to volatilize and remove the organic solvent. The nanomedicine of the present invention can be obtained after centrifugal separation, washing with deionized water, and freeze-drying.

Embodiment 3

[0040] First, 4 mg of lecithin and 6 mg of polyethylene glycol-distearoyl phosphatidyl ethanolamine (wherein the molecular weight of polyvinyl alcohol is 2000 Da) was dissolved in 10 mL of double distilled water under the condition of constant temperature magnetic stirring at 65 ° C, until the solid matter was completely dissolved, Let cool to room temperature. 30 mg of 4-hydroxymethylbenzeneboronic acid pinacol ester modified β-cyclodextrin derivative and 10 mg of 4-amino-2,2,6,6-tetramethylpiperidine oxide were dissolved in 1.2mL methanol / in dimethylformamide. The organic phase was then slowly added dropwise to the aqueous phase (1 mL / min) with stirring. After the dropwise addition was completed, stirring was continued at 60° C. for 8 h to volatilize and remove the organic solvent. The nanomedicine of the present invention can be obtained after centrifugal separation, washing with deionized water, and freeze-drying.

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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 nanomedicine for resisting oxidative stress injury, in particular to the composition and preparation of a nanomedicine simulating superoxide dismutase / catalase and its use in preventing and treating inflammatory bowel disease and other oxidative stress-related diseases applications in . 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, which mainly includes two clinical manifestations, Crohn's disease and nonspecific ulcerative colitis, which seriously affects human health. Although the exact cause of IBD is still unclear, there is abundant evidence that genetic factors, immune system, and environmental facto...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K45/06A61K9/19A61K31/724A61K47/34A61K47/24A61P1/00A61P9/04A61P9/10A61P39/06A61K31/445
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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