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Thrombus targeting long circulating polycation micelle, and preparation method and applications thereof

A polycationic, long-circulating technology, applied in the field of medicine, can solve problems such as unreported, and achieve the effects of reducing immunogenicity, prolonging in vivo action time, and obvious thrombus targeting.

Pending Publication Date: 2021-04-09
XIAN MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Therefore, the construction of RGD peptide-modified PEOz-chitosan polycation micelles is expected to achieve anticoagulation and antithrombotic thrombus targeting and long-term circulation in vivo. At present, RGD-PEOz-chitosan polycation micelles and their applications Thrombosis targeted therapy has not been reported yet

Method used

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  • Thrombus targeting long circulating polycation micelle, and preparation method and applications thereof
  • Thrombus targeting long circulating polycation micelle, and preparation method and applications thereof
  • Thrombus targeting long circulating polycation micelle, and preparation method and applications thereof

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preparation example Construction

[0029] A method for preparing a thrombus-targeted long-circulating polycationic micelle, which specifically comprises the following steps:

[0030] Step 1. Take anhydrous EOz and place it in a round-bottomed flask, add 80-250 mL of anhydrous acetonitrile, add 3-bromo-ethyl propionate and potassium iodide according to the molecular weight of the polymer to be synthesized according to the ratio of monomer and initiator, The mass ratio of anhydrous EOz to 3-bromo-ethyl propionate is 1~5:1, and the molar ratio of 3-bromo-ethyl propionate to potassium iodide is 1:0.5~2, stirring under nitrogen protection, 80~120 The temperature is heated to reflux for 24-48h, and the stirring speed is 300-800rpm. After the reaction solution is cooled to room temperature, potassium hydroxide methanol solution is added to terminate the reaction. The molar ratio of potassium hydroxide to 3-bromo-ethyl propionate is 2-5 : 1, 80-120 ℃ heating under reflux for 12-24 h, the organic solvent in the reaction...

Embodiment 1

[0043] Step 1, Synthesis of HOOC-PEOZ-OH

[0044] Take 10g of anhydrous EOz and place it in a round-bottomed flask, add 80mL of anhydrous acetonitrile, add 3-bromo-ethyl propionate and potassium iodide (mol ratio 1:0.5) according to the mass ratio of monomer and initiator to be 1:1, Stir under nitrogen protection (300rpm), heat under reflux at 80°C for 24h, and after the reaction solution is cooled to room temperature, add potassium hydroxide methanol solution to terminate the reaction (the molar ratio of potassium hydroxide to 3-bromo-ethyl propionate is 1 : 1), heated to reflux at 80 °C for 12 h, removed the organic solvent in the reaction solution by rotary evaporation at 40 °C, reconstituted with 10 mL of dichloromethane, precipitated with 200 mL of cold ether, and filtered with suction. The obtained solid was dissolved in 10 mL of water, placed in a dialysis bag with a molecular weight of 8000, dialyzed in deionized water for 24 hours, and freeze-dried for 1 day to obtain...

Embodiment 2

[0055] Step 2, Synthesis of HOOC-PEOZ-OH

[0056] Take 15g of anhydrous EOz and place it in a round-bottomed flask, add 100mL of anhydrous acetonitrile, according to the mass ratio of monomer and initiator to be 2:1, add 3-bromo-ethyl propionate and potassium iodide (mol ratio 1:1) , stirred under nitrogen protection (400rpm), heated and refluxed at 100°C for 36h, and after the reaction solution was cooled to room temperature, potassium hydroxide methanol solution was added to terminate the reaction (the molar ratio of potassium hydroxide to 3-bromo-ethyl propionate was 2:1), heated to reflux at 100°C for 12h. The organic solvent in the reaction solution was removed by rotary evaporation at 50°C, redissolved with 12 mL of dichloromethane, precipitated with 250 mL of cold ether, and filtered with suction. The obtained solid was dissolved in 15 mL of water, placed in a dialysis bag with a molecular weight of 10,000, dialyzed in deionized water for 36 h, and freeze-dried for 1 d...

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Abstract

The invention discloses a thrombus targeting long circulating polycation micelle, and a preparation method and applications thereof. Through an EDC / NSH esterification system, poly(2-ethyl-2-oxazoline) is used to graft chitosan so as to prepare the polyion micelle; modification is performed on chain ends by using arginine-glycine-aspartic acid sequence short peptide; and through the carrying of anticoagulant and antithrombotic drugs, the thrombus targeting long circulating polycation micelle can be obtained. Through the prepared thrombus targeting polyion micelle, the purposes of improving protein drug stability, targeting thrombus, prolonging the action time in vivo and reducing immunogenicity can be achieved. The preparation method is feasible and reliable in operation; the obtained carrier is high in drug loading; the drugs have obvious thrombus targeting performance and are long in action time in vivo; and therefore, theoretical basis can be provided for the research of a novel thrombus targeting delivery system.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a thrombus-targeted long-circulation polycation micelle, and also relates to a preparation method and application of the micelle. Background technique [0002] Cardiovascular and cerebrovascular diseases are the most lethal diseases today, seriously threatening human life and health. Ischemic stroke, myocardial infarction and venous thromboembolism caused by thrombus are the three major killers of cardiovascular and cerebrovascular diseases. Drug thrombolysis is a common method of clinical thrombosis treatment. However, anticoagulant and antithrombotic drugs lack tissue specificity, cannot selectively act on lesion sites, and are prone to serious complications such as bleeding. These shortcomings greatly limit their clinical application. Therefore, research on new drug delivery systems for anticoagulant and antithrombotic drugs has attracted the attention of many s...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K31/727A61K38/58A61K45/00A61K47/36A61K47/62A61P7/02
CPCA61K9/1075A61K31/727A61K38/58A61K45/00A61K47/36A61K47/62A61P7/02
Inventor 王小宁梁晓燕闫梦茹马远涛高迎春赵宁
Owner XIAN MEDICAL UNIV
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