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Quercetin-modified nano sulfur as well as preparation method and application thereof to anti-AD (Alzheimer's Disease) drug

A technology of quercetin and nano-sulfur, which is applied in the directions of drug combination, drug delivery, and medical preparations of inactive ingredients, etc., can solve the problems of reducing drug efficacy and low blood-brain barrier permeability, and achieves improving drug efficacy, inhibiting Effects of endoplasmic reticulum stress, high biocompatibility

Active Publication Date: 2018-11-13
JINAN UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

General AD treatment drugs have low penetration ability to the blood-brain barrier (BBB), thus limiting their effect on the brain of patients and reducing drug efficacy

Method used

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  • Quercetin-modified nano sulfur as well as preparation method and application thereof to anti-AD (Alzheimer's Disease) drug
  • Quercetin-modified nano sulfur as well as preparation method and application thereof to anti-AD (Alzheimer's Disease) drug
  • Quercetin-modified nano sulfur as well as preparation method and application thereof to anti-AD (Alzheimer's Disease) drug

Examples

Experimental program
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Effect test

Embodiment 1

[0049] This embodiment provides a quercetin-modified nano-sulfur and its preparation method, as well as a pharmaceutical preparation containing the quercetin-modified nano-sulfur and its preparation method.

[0050] A quercetin-modified nano sulfur and preparation method thereof:

[0051] Mix 2.5 mL of quercetin aqueous solution with a concentration of 4 mM and 2.5 mL of an aqueous solution of methionine with a concentration of 100 mM, add 2 mL of an aqueous solution of vitamin C (Vc) with a concentration of 0.1 M, and then slowly drop 5 mL of methionine with a concentration of 10 mM Sodium thiosulfate solution to obtain a mixed solution, react, observe that the color of the solution changes from transparent to light white, continue the ultrasonic reaction for 20min, centrifuge to obtain a precipitate, wash three times with distilled water, and obtain quercetin-modified nano-sulfur (Qc@SNPs ).

[0052] A pharmaceutical preparation containing the quercetin-modified nano-sulfur...

Embodiment 2

[0058] This embodiment provides a quercetin-modified nano-sulfur and its preparation method, as well as a pharmaceutical preparation containing the quercetin-modified nano-sulfur and its preparation method.

[0059] Mix 2.5mL of quercetin aqueous solution with a concentration of 3.2mM and 2.4mL of methionine aqueous solution with a concentration of 50mM, add 1.8mL of vitamin C (Vc) aqueous solution with a concentration of 0.05M, and slowly drop 5mL of 6mM sodium thiosulfate solution to obtain a mixed solution, react, and observe that the color of the solution changes from transparent to light white, continue the ultrasonic reaction for 15min, centrifuge to obtain a precipitate, wash three times with distilled water, and obtain quercetin-modified nano-sulfur (Qc @SNPs).

[0060] A pharmaceutical preparation containing the quercetin-modified nano-sulfur and a preparation method thereof:

[0061] Add 30 mL of quercetin-modified nano-sulfur aqueous solution with a concentration o...

Embodiment 3

[0063] This embodiment provides a quercetin-modified nano-sulfur and its preparation method, as well as a pharmaceutical preparation containing the quercetin-modified nano-sulfur and its preparation method.

[0064] Mix 2.5mL of quercetin aqueous solution with a concentration of 5mM and 2.5mL of methionine aqueous solution with a concentration of 180mM, add 2mL of vitamin C (Vc) aqueous solution with a concentration of 0.3M, and slowly drop 5mL of methionine with a concentration of 15mM under ultrasonic conditions. Sodium thiosulfate solution to obtain a mixed solution, react, observe that the color of the solution changes from transparent to light white, continue the ultrasonic reaction for 30min, centrifuge to obtain a precipitate, wash three times with distilled water, and obtain quercetin-modified nano-sulfur (Qc@SNPs ).

[0065] A pharmaceutical preparation containing the quercetin-modified nano-sulfur and a preparation method thereof:

[0066] Add 30 mL of quercetin-mod...

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Abstract

The invention belongs to the technical field of preparation of drugs, and specifically relates to quercetin-modified nano sulfur as well as a preparation method and application thereof to an anti-AD (Alzheimer's Disease) drug. According to the preparation method disclosed by the invention, quercetin is modified on nano sulfur by utilizing the microsize and a high surface energy effect of nano sulfur, not only a function of the quercetin for reducing endoplasmic reticulum stress in cells of the quercetin is utilized, but also the water solubility is improved, so that quercetin-modified nano sulfur integrating high biocompatibility and an AD treatment effect is obtained. The quercetin-modified nano sulfur is further embedded in a microbubble shell prepared from alpha-butyl cyanoacrylate by adopting a one-pot method, so that a drug preparation containing quercetin-modified nano sulfur is prepared; microbubbles of the drug preparation can be destroyed under ultrasonic action, sonoporationcan be generated, a blood brain barrier can be temporarily opened, and quercetin-modified nano sulfur can further enter the brain by penetrating through the blood brain barrier so as to take a treatment effect, so that high brain targeting performance is obtained. The preparation method of the drug preparation is simple, and products are convenient to preserve and use.

Description

technical field [0001] The invention belongs to the technical field of medicine preparation, and in particular relates to quercetin-modified nano-sulfur, its preparation method and its application in anti-Alzheimer's disease medicine. Background technique [0002] Alzheimer's disease (AD) is a common neurodegenerative disease. Because its pathogenesis is very complex, its therapeutic drugs are very limited, and its treatment is still difficult. Currently, there are two main mechanisms of the recognized pathogenesis of Alzheimer's disease. First, the abnormal aggregation of amyloid (Aβ) is considered to be closely related to the pathogenesis of AD. Second, the endoplasmic reticulum is an important organelle responsible for the processing and folding of proteins, such as the formation of disulfide bonds and glycosylation of proteins. However, when the internal and external environment of the cell is disturbed, the unfolded protein response (UPR) or misfolded proteins will a...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/55A61K33/04A61P25/28A61K9/127A61K47/32A61K41/00A61K31/352
CPCA61K9/0009A61K9/1273A61K31/352A61K33/04A61K41/0028A61K47/32A61K47/55A61P25/28A61K2300/00
Inventor 刘杰谢文杰
Owner JINAN UNIVERSITY
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