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Method for constructing ordered ischemic-cardiomyocyte-mitochondria-targeting drug-loading nanometer micelle

A drug-loaded nano-cardiomyocyte technology, which is applied in the fields of pharmaceutical formulations, drug combinations, cardiovascular system diseases, etc., can solve problems such as low concentration, lack of tissue specificity, and unsatisfactory expected drug efficacy.

Active Publication Date: 2018-09-18
THE SECOND XIANGYA HOSPITAL OF CENT SOUTH UNIV
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  • Claims
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Problems solved by technology

At present, most of the drugs used in the clinical treatment of myocardial I / R injury lack tissue specificity, are not very selective for cardiomyocytes, and reach the mitochondrial effect target at a very low concentration, resulting in unsatisfactory expected efficacy of the drug

Method used

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  • Method for constructing ordered ischemic-cardiomyocyte-mitochondria-targeting drug-loading nanometer micelle
  • Method for constructing ordered ischemic-cardiomyocyte-mitochondria-targeting drug-loading nanometer micelle
  • Method for constructing ordered ischemic-cardiomyocyte-mitochondria-targeting drug-loading nanometer micelle

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specific Embodiment approach

[0033] The specific embodiment (raw materials and reagents not specified in the examples are all commercially available)

[0034] Taking the method of constructing puerarin-loaded order-level targeted nanomicelles as an example, it includes the following steps:

[0035] (1) Synthesis of TPP-PEG-PE block copolymer:

[0036] Accurately weigh 100mg (0.23mM) CTPP dissolved in 10mL chloroform, add 200μL triethylamine, 124mg (0.64mM) EDC and 74mg (0.64mM) NHS, stir at room temperature for 2h, then add 25mL concentration of 25mg / mL DSPE- PEG-NH 2 (Molecular weight: 2790, 0.22mM) in chloroform solution, under the protection of nitrogen, stirred at room temperature overnight, the crude reactant was washed with glacial ether for several times, centrifuged to remove the lower precipitate, and then freeze-dried to obtain TPP-PEG-PE embedded segment copolymer, the specific synthetic route is as follows:

[0037]

[0038] (2) Preparation of sequence-targeted nanomicelles loaded with p...

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Abstract

The invention discloses a method for constructing an ordered ischemic-cardiomyocyte-mitochondria-targeting drug-loading (model drugs such as puerarin, baicalin, and the like respectively can act on ischemic cardiomyocyte mitochondria so as to treat myocardial ischemia reperfusion injury ) nanometer micelle, wherein the method comprises synthesizing a TPP-PEG-PE block copolymer, and preparing an ordered targeting drug-loaded nanometer micelle. According to the present invention, the puerarin drug is precisely delivered to ischemic cardiomyocyte mitochondria by using the ordered targeting drug-loaded nanometer micelle so as to provide the pharmacological effect, wherein the drug carrier is accumulated in the ischemic myocardium at the early stage of the infarct in a targeting manner throughthe EPR effect of the PEG-PE nanometer micelle, and the charge effect of the TPP cation mediates the drug carrier to enter the negatively charged cardiomyocyte mitochondria to deliver the puerarin andother drugs to the ischemic cardiomyocyte mitochondria in stages so as to achieve the precise administration.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a method for constructing sequence-level drug-loaded nanomicelles targeting ischemic cardiomyocyte mitochondria. Background technique [0002] Acute myocardial infarction (AMI) is a common clinical emergency that can lead to sudden death of patients. Coronary intervention to restore coronary blood flow is a common clinical treatment for AMI patients, but the resulting myocardial ischemia / reperfusion (I / R) injury can increase the size of ischemic myocardial infarction. Increase 20%-50%, there is no good solution at present. The mechanism of myocardial I / R injury is mainly manifested as mitochondrial dysfunction, and the induction of myocardial cell apoptosis and autophagy. Restoring the normal function of mitochondria is undoubtedly of great scientific research value for alleviating myocardial I / R injury. At present, most of the drugs used clinically to tre...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K31/352A61K31/7048A61K47/24A61P9/10
CPCA61K9/1075A61K31/352A61K31/7048A61K47/24A61P9/10
Inventor 刘新义向大雄李文群罗世林杨永玉李健和胡雄彬
Owner THE SECOND XIANGYA HOSPITAL OF CENT SOUTH UNIV
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