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Nanometer carrier for targeting treatment of myocardial injury and application thereof

A nano-carrier and targeted therapy technology, applied in the field of biomedicine, can solve problems such as damage to heart function, limit the efficiency of stem cell transplantation treatment, and have no specificity, and achieve the effect of reducing side effects

Active Publication Date: 2019-04-12
深圳市孙逸仙心血管医院
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Traditional drug therapy and surgical treatment have seriously reduced the mortality rate of myocardial infarction, but the infarcted cardiomyocytes cannot regenerate, thereby impairing the function of the heart
Furthermore, stem cells transplanted in ischemic heart tissue are affected by apoptosis and necrosis due to the oxidative and inflammatory microenvironment of the infarct zone, severely limiting the therapeutic efficiency of stem cell transplantation
Traditional nanomaterials have no specificity when carrying drugs, which leads to certain toxic side effects on normal cells

Method used

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  • Nanometer carrier for targeting treatment of myocardial injury and application thereof
  • Nanometer carrier for targeting treatment of myocardial injury and application thereof
  • Nanometer carrier for targeting treatment of myocardial injury and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] This embodiment provides a method for preparing a tanshinone IIA-loaded nanocarrier, which sequentially includes the following steps:

[0041] S1) Dissolve carboxyl-salted polylactic acid-glycolic acid in dichloromethane, then add N-hydroxysuccinimide and 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide salt Acid salt, activated to produce polylactic acid-glycolic acid-N-hydroxysuccinimide; after the activation reaction, followed by precipitation with ice ether, dialysis and vacuum drying; the abbreviation of polylactic acid-glycolic acid-N-hydroxysuccinimide PLG-NHS, PLG-NHS is a polymer of the structure represented by formula (I);

[0042]

[0043] Among them, n≥2;

[0044] S2) Dissolve PLG-NHS into chloroform, add aminopolyethylene glycol carboxyl group and N,N-diisopropylethylamine to activate it to form polylactic acid-glycolic acid-polyethylene glycol; after the activation reaction, Then carry out ice methanol precipitation, ice methanol washing and vacuum drying in seque...

Embodiment 2

[0056] This embodiment provides a method for preparing tanshinone IIA-loaded nanocarriers. The differences from Embodiment 1 are:

[0057] 1) In step S1, the amount ratio of polylactic acid-glycolic acid, N-hydroxysuccinimide and 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride is 0.1:10:1, the total volume of dichloromethane, polylactic acid-glycolic acid, N-hydroxysuccinimide and 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride and The volume ratio of dichloromethane is 5:1, the activation reaction time is 4h, dichloromethane, polylactic acid-glycolic acid, N-hydroxysuccinimide and 1-(3-dimethylaminopropyl)-3- The ratio of the total volume of ethylcarbodiimide hydrochloride to the volume of glacial ether is 1:10, dialysis adopts a dialysis bag with a molecular weight cut-off of 500, the temperature of vacuum drying is 50℃, and the time of vacuum drying is 19h;

[0058] 2) In step S2, the ratio of PLGA-NHS to N,N-diisopropylethylamine is 1:5, the activation ...

Embodiment 3

[0062] This embodiment provides a method for preparing tanshinone IIA-loaded nanocarriers. The differences from Embodiment 1 are:

[0063] 1) In step S1, the amount ratio of polylactic acid-glycolic acid, N-hydroxysuccinimide and 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride is 1:1:1, the total volume of dichloromethane, polylactic acid-glycolic acid, N-hydroxysuccinimide and 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride and The volume ratio of dichloromethane is 20:1, the activation reaction time is 12h, dichloromethane, polylactic acid-glycolic acid, N-hydroxysuccinimide and 1-(3-dimethylaminopropyl)-3- The ratio of the total volume of ethylcarbodiimide hydrochloride to the volume of glacial ether is 1:20, dialysis adopts a dialysis bag with a molecular weight cut-off of 3500, the temperature of vacuum drying is 60℃, and the time of vacuum drying is 12h;

[0064] 2) In step S2, the ratio of PLGA-NHS to N,N-diisopropylethylamine is 1:10, the activation...

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Abstract

The invention discloses a nanometer carrier for targeting treatment of myocardial injury and an application thereof, belonging to the technical field of biomedical technology, wherein the nanometer carrier is polylactic acid-glycolic acid-polyethylene glycol-atrial natriuretic peptide or its pharmaceutical acid addition salt, nano-carrier and tanshinone IIA can prepare the nanometer composite PLGA-PEG-ANP / TAN loaded with tanshinone IIA. As that nano-composite carry out targeted repair on the heart injury after myocardial infarction, the side effects of tanshinone IIA on other tissue cells canbe reduced, and the tanshinone IIA can be released appropriately.

Description

Technical field [0001] The invention belongs to the technical field of biomedicine, and in particular relates to a nano carrier for targeted treatment of myocardial injury and its application. Background technique [0002] Myocardial infarction is the main cause of mortality and morbidity worldwide. Myocardial infarction can cause the loss of up to 1 billion cardiomyocytes. Due to the very limited regeneration capacity of myocardium after injury, the lost cells are replaced by fibrotic scar tissue, leading to heart failure. Although surgical treatment reduces the mortality associated with myocardial infarction, the infarcted myocardial cells cannot regenerate, thereby impairing heart function. Although a lot of efforts have been made to prevent, limit or treat heart failure, so far, there is still no treatment that can successfully restore the function of the injured heart. [0003] According to reports, small drug molecules may be used for myocardial production. In the past few...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08G81/00A61K9/107A61K31/58A61K47/42A61P9/00A61P9/10
CPCA61K9/1075A61K31/58A61K47/42A61P9/00A61P9/10C08G81/00
Inventor 柯晓彭长农王小庆
Owner 深圳市孙逸仙心血管医院