Drug-loaded polymer micelle for treating cardiovascular diseases and preparation method and application thereof

A technology of drug-loaded polymers and polymer glues, which can be used in cardiovascular system diseases, drug combinations, and pharmaceutical formulations. narrow effect

Inactive Publication Date: 2019-07-12
SOUTHWEST JIAOTONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0003] However, when bare metal stents are implanted into patients with atherosclerosis, not only will there be inflammatory reactions, but also complications such as intravascular restenosis and late thrombosis will occur in the late stage, which hinders the development of stents.

Method used

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  • Drug-loaded polymer micelle for treating cardiovascular diseases and preparation method and application thereof
  • Drug-loaded polymer micelle for treating cardiovascular diseases and preparation method and application thereof
  • Drug-loaded polymer micelle for treating cardiovascular diseases and preparation method and application thereof

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preparation example Construction

[0034] The embodiment of the present invention also provides a preparation method of the above-mentioned drug-loaded polymer micelles for treating cardiovascular diseases, the preparation method comprising the following steps:

[0035] Micellar extraction of a novel hydrogen sulfide-releasing form of aspirin using a solution containing polymeric micelles followed by isolation.

[0036] The preparation method of the polymer micelle comprises: dissolving the polymer in an organic solvent to obtain a polymer solution; under ultrasonic conditions, adding the polymer solution dropwise into deionized water, followed by dialysis with deionized water, through Dried to obtain polymer micelles;

[0037] Preferably, the organic solvent is selected from at least one of DMF and DMAC;

[0038] Preferably, the concentration of the polymer solution is 8-12 mg / mL, more preferably 10 mg / mL;

[0039] Preferably, the volume ratio of the polymer solution to the deionized water is 1:(8-16), more pr...

Embodiment 1

[0063] An embodiment of the present invention provides a drug-loaded polymer micelle for treating cardiovascular diseases.

[0064] Synthetic steps of polymer micelles:

[0065] 1.HO(CH 2 ) 11 SeSe(CH 2 ) 11 The preparation steps of OH (bis(11-hydroxyl undecyl) diselenide):

[0066] Sodium borohydride (NaBH 4 ) is dissolved in deionized water, and reacts with selenium powder to generate hydrogen gas and colorless solution sodium diselenide (Na 2 Se 2 ). The mass ratio of sodium borohydride to selenium powder is 2:1; it should be noted that, in other embodiments, the mass ratio of sodium borohydride to selenium powder can be selected within the range of (1.5-2):1.

[0067] Under argon protection, sodium diselenide and 11-bromoundecanol (Br(CH 2 ) 11 OH) in the organic solvent anhydrous tetrahydrofuran (THF) for substitution reaction, the substitution reaction time is 12h, the substitution reaction temperature is 50°C, and then the substitution reaction product is sepa...

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Abstract

The invention discloses a drug-loaded polymer micelle for treating cardiovascular diseases and a preparation method and application thereof, and relates to the technical field of cardiovascular therapy. In particular, the polymer micelle is encapsulated with a novel hydrogen sulfide release aspirin, can be applied to a cardiovascular pathological change environment with a low pH and high oxidativestress environment, has a balanced regulation function on vascular physiology, and can be used for long-acting, sustained-release and targeted treatment of the cardiovascular diseases; in particular,the drug-loaded polymer micelles is expected to reduce or avoid the risks of intravascular restenosis, endothelium delayed healing and late thrombosis.

Description

technical field [0001] The present invention relates to the technical field of cardiovascular treatment, in particular to a drug-loaded polymer micelle for treating cardiovascular diseases and its preparation method and application. Background technique [0002] Cardiovascular disease is currently the technology with the highest morbidity and mortality among all diseases, higher than tumors and other diseases, and poses a great threat to human health. Among cardiovascular diseases, coronary heart disease is a very harmful one, and atherosclerosis is the basic cause of coronary heart disease. Percutaneous coronary intervention can restore the normal flow of blood in blood vessels, and it is the main way to treat atherosclerosis clinically, and it has been widely used clinically. [0003] However, when bare metal stents are implanted into patients with atherosclerosis, not only inflammation will occur, but also complications such as intravascular restenosis and late thrombosi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K47/34A61K31/616A61P9/00A61P9/10
CPCA61K9/1075A61K31/616A61K47/34A61P9/00A61P9/10
Inventor 赵安莎罗丹路槟阳杨苹
Owner SOUTHWEST JIAOTONG UNIV
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