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Two-stage targeted polymeric pro-drug for treating acute kidney injury and preparation method

A technology for acute kidney injury and prodrugs, applied in the field of new drug delivery system research, can solve the problems of poor water solubility, poor stability, and limited clinical application, and achieve the effect of reversing oxidative stress damage and increasing distribution

Active Publication Date: 2020-02-21
NINGBO UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, its poor water solubility, poor stability and low bioavailability greatly limit its clinical application.

Method used

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  • Two-stage targeted polymeric pro-drug for treating acute kidney injury and preparation method
  • Two-stage targeted polymeric pro-drug for treating acute kidney injury and preparation method
  • Two-stage targeted polymeric pro-drug for treating acute kidney injury and preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] 1. Synthesis of (4-carboxybutyl)triphenylphosphonium bromide-low molecular weight chitosan graft

[0041] Weigh 0.8866g (4-carboxybutyl) triphenylphosphonium bromide and add it to 10mL thionyl chloride, then add 50 μL N,N-dimethylformamide, stir at 90℃ to completely dissolve and condense the reactants Reflux and react for 4h to activate the carboxyl group of (4-carboxybutyl)triphenylphosphonium bromide. After the solvent is removed by rotary evaporation, 6.448g of low molecular weight chitosan (polymerization degree 40) is added to the round bottom flask and added 10mL anhydrous dimethyl sulfoxide solution, continue to react for 48h. After the reaction, the reaction product was placed in a dialysis bag with a molecular weight cut-off of 1000, and the dialysis was continued with pure water for 48 hours. The suspension in the dialysis bag was collected, centrifuged at 14000 rpm for 10 min, and the supernatant was taken to freeze-dry to obtain (4-carboxybutyl)triphenylphosph...

Embodiment 2

[0044] 1. Synthesis of (4-carboxybutyl)triphenylphosphonium bromide-low molecular weight chitosan graft

[0045] Weigh 0.8866g (4-carboxybutyl) triphenylphosphonium bromide and add it to 10mL thionyl chloride, then add 50 μL N,N-dimethylformamide, stir at 90℃ to completely dissolve and condense the reactants Reflux and react for 4h to activate the carboxyl group of (4-carboxybutyl)triphenylphosphonium bromide. After the solvent is removed by rotary evaporation, 4.836g of low molecular weight chitosan (polymerization degree 30) is added to the round bottom flask and added 10mL anhydrous dimethyl sulfoxide solution, continue to react for 48h. After the reaction, the reaction product was placed in a dialysis bag with a molecular weight cut-off of 1000, and the dialysis was continued with pure water for 48 hours. The suspension in the dialysis bag was collected, centrifuged at 14000 rpm for 10 min, and the supernatant was taken to freeze-dry to obtain (4-carboxybutyl)triphenylphosph...

Embodiment 3

[0048] 1. Synthesis of (4-carboxybutyl)triphenylphosphonium bromide-low molecular weight chitosan graft

[0049] Weigh 0.8866g (4-carboxybutyl) triphenylphosphonium bromide and add it to 10mL thionyl chloride, then add 50 μL N,N-dimethylformamide, stir at 90℃ to completely dissolve and condense the reactants Reflux and react for 4h to activate the carboxyl group of (4-carboxybutyl)triphenylphosphonium bromide. After the solvent is removed by rotary evaporation, 3.224g of low molecular weight chitosan (polymerization degree 20) is added to the round bottom flask and added 10mL anhydrous dimethyl sulfoxide solution, continue to react for 48h. After the reaction, the reaction product was placed in a dialysis bag with a molecular weight cut-off of 1000, and the dialysis was continued with pure water for 48 hours. The suspension in the dialysis bag was collected, centrifuged at 14000 rpm for 10 min, and the supernatant was taken to freeze-dry to obtain (4-carboxybutyl)triphenylphosph...

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PUM

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Abstract

The invention discloses a two-stage targeted polymeric pro-drug for treating acute kidney injury and a preparation method and belongs to the field of medicines. The polymeric pro-drug is prepared by grafting (4-carboxybutyl) triphenyl phosphonium bromide, curcumin and low molecular weight chitosan of different polymerization degrees. According to the polymeric pro-drug, the low molecular weight chitosan is combined with a Megalin receptor which is specifically expressed on the surface of renal tubular epithelial cells, and distribution of the curcumin in target cells is increased; under medication of mitochondrion target molecules (4-carboxybutyl) triphenyl phosphonium bromide, the polymeric pro-drug fed into cells further increases distribution of the curcumin in target cell mitochondria,and by reducing ROS (reactive oxygen species) generated by the mitochondria, oxidative stress injury of the renal tubular epithelial cells can be effectively reversed, and targeted therapy on ischemia reperfusion injury can be achieved.

Description

Technical field [0001] The invention belongs to the research field of new drug delivery systems, and particularly relates to a two-stage targeting polymer prodrug for treating acute kidney injury and a preparation method. Background technique [0002] Acute kidney injury refers to a clinical syndrome in which a variety of invasive factors (such as ischemia-reperfusion injury, endotoxin, drugs, etc.) cause renal function to decline acutely in a short period of time, including renal function from minor changes to final renal failure. During the process, the onset was rapid and the mortality rate was as high as 60.3% (52% of them died in ICU). Although the medical treatment and blood purification treatment of acute kidney injury are constantly improving, the morbidity and mortality of the disease are still very high, which makes clinicians around the world pay more and more attention to acute kidney injury, aiming to find Effective treatment methods intervene and curb the disease p...

Claims

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Application Information

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IPC IPC(8): A61K47/61A61K31/12A61P13/12C08B37/08
CPCA61K47/61A61K31/12A61P13/12C08B37/003
Inventor 胡静波王东伟谭学莹李淑娟赵玉芬
Owner NINGBO UNIV
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