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Preparation method of pH-sensitive lutein-chitosan nano-micelle loaded with tripterine

A nanotechnology of tripterine and chitosan, which is applied in the field of medicine, can solve the problems of low bioavailability, achieve simple preparation methods, improve the microenvironment of kidney inflammation, and improve the effect of AKI

Pending Publication Date: 2022-03-15
THE FIRST AFFILIATED HOSPITAL OF HENAN UNIV OF TCM
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] For above-mentioned situation, in order to solve the defective of prior art, the purpose of the present invention is exactly to provide a kind of preparation method of the lutein-chitosan nano-micelle that loads tripterine pH sensitivity, can effectively solve the biological problem of LU and Cel. Low utilization, reducing the toxicity of Cel to vital organs such as the heart, liver and nervous system

Method used

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  • Preparation method of pH-sensitive lutein-chitosan nano-micelle loaded with tripterine
  • Preparation method of pH-sensitive lutein-chitosan nano-micelle loaded with tripterine

Examples

Experimental program
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Effect test

Embodiment 1

[0025] When the present invention is implemented, the preparation method of the nano micelles specifically comprises the following steps:

[0026] 1) Synthesis of pH-responsive excipients and lutein covalently coupled compounds:

[0027] Weigh 150mg of lutein into a round bottom flask, fully dissolve in anhydrous dichloromethane, then add 2mL of pH-responsive auxiliary material propionic anhydride, and finally slowly add 0.1mL of organic solvent anhydrous pyridine dropwise. Under the protection of nitrogen, react at room temperature and avoid light for 12 hours. After the reaction, wash with dichloromethane, extract repeatedly with 2mol / L acidic solvent glacial acetic acid, and finally extract twice with 10mL saturated calcium chloride solution, combine the organic phases, and then add anhydrous chlorine Calcium chloride solid, dried overnight to absorb excess water in the sample, filtered and concentrated to obtain a yellow extract product for column chromatography separation...

Embodiment 2

[0033] When the present invention is implemented, the preparation method of the nano micelles specifically comprises the following steps:

[0034] 1) Synthesis of pH-responsive excipients and lutein covalently coupled compounds:

[0035]Weigh 200 mg of lutein in a round bottom flask, fully dissolve in anhydrous dichloromethane, then add 5 mL of pH-responsive auxiliary material citraconic anhydride, and finally slowly add 0.2 mL of organic solvent triethylamine, and react for 24 hours at room temperature under nitrogen protection. After the reaction, wash with dichloromethane, repeatedly extract with 2mol / L acidic solvent glacial hydrochloric acid, and finally extract 4 times with 20mL saturated sodium chloride, combine the organic phases, then add anhydrous magnesium sulfate, and dry overnight to absorb the excess in the sample. Water, filtered and concentrated to obtain a yellow extract product for column chromatography separation, the concentrated sample was loaded, purified...

Embodiment 3

[0041] When the present invention is implemented, the preparation method of the nano micelles specifically comprises the following steps:

[0042] 1) Synthesis of pH-responsive excipients and lutein covalently coupled compounds:

[0043] Weigh 300mg of lutein in a round bottom flask, fully dissolve in anhydrous dichloromethane, then add 6mL of pH responsive auxiliary material citraconic anhydride, and finally slowly add 0.3mL of organic solvent toluene, react at room temperature and avoid light for 24 hours under nitrogen protection, and the reaction is over Finally, wash with dichloromethane, extract repeatedly with 4mol / L acidic solvent glacial acetic acid, and finally extract 6 times with 15mL saturated sodium chloride solution, combine the organic phases, then add solid desiccant sodium hydroxide, and dry overnight to absorb the Excess water, filtered and concentrated to obtain a yellow extract product for column chromatography separation, concentrated sample loading, puri...

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Abstract

The invention relates to a preparation method of tripterine-loaded pH-sensitive lutein-chitosan nano-micelles, which can effectively solve the problems of low bioavailability of LU and Cel and reduction of toxicity of Cel to important organs such as heart, liver and nervous system, and adopts the technical scheme that the tripterine-loaded pH-sensitive lutein-chitosan nano-micelles can be used for preparing the tripterine-loaded pH-sensitive lutein-chitosan nano-micelles. The specific preparation method comprises the following steps: (1) synthesizing a covalent coupling compound of the pH response auxiliary material and the xanthophyll; (2) preparing a lutein-chitosan polymer which is sensitive to pH (Potential of Hydrogen); 3) preparation of the pH-sensitive lutein-chitosan nano delivery system loaded with the tripterine, the preparation method is simple, the prepared pH-sensitive lutein-chitosan nano delivery system loaded with the tripterine can effectively respond to the acid environment of lysosome in renal tubular epithelial cells, the lutein and the tripterine are released, and the delivery effect is good. Kidney inflammation microenvironment can be rapidly improved, AKI can be improved, and the traditional Chinese medicine composition is an innovation of pharmaceutical preparations for treating AKI.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a preparation method of pH-sensitive lutein-chitosan nano-micelle loaded with tripterine. Background technique [0002] Acute kidney injury (Acute Kidney Injury, AKI) is a short-term, rapid onset of renal insufficiency syndrome. It causes 2 million deaths worldwide every year, is characterized by sudden deterioration of renal function and rapid apoptosis of renal tubular cells, and is characterized by high morbidity and mortality. When AKI occurs, the content of reactive oxygen species (ROS) in the kidney increases explosively, further stimulating cells to produce a large number of inflammatory factors, and rapidly causing AKI. Therefore, it is of great significance to improve the therapeutic effect of AKI. [0003] According to literature reports, lutein (Lutein, LU) is a kind of carotenoid, which has the characteristics of high efficiency, non-toxicity and anti-oxidation. The antioxi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/047A61K47/61A61P13/12
CPCA61K31/047A61K47/61A61P13/12
Inventor 赵娅杜斌于利利唐进法段松超杨亚蕾
Owner THE FIRST AFFILIATED HOSPITAL OF HENAN UNIV OF TCM
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