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A kind of paeonol-ozagrel conjugate brain targeting liposome and preparation method thereof

A technology of conjugates and paeonol, which is applied in the field of paeonol-ozagrel conjugated brain-targeted liposomes and its preparation, can solve the problem of achieving effective therapeutic concentrations, complex brain structures, and difficulties in active drugs. and other problems, to achieve the effect of high encapsulation rate, prolong cycle time, and avoid phagocytosis

Active Publication Date: 2021-07-27
ANHUI UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition, the structure of the brain is complex, and it is difficult for most active drugs to reach effective therapeutic concentrations in the brain through the blood-brain barrier.

Method used

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  • A kind of paeonol-ozagrel conjugate brain targeting liposome and preparation method thereof
  • A kind of paeonol-ozagrel conjugate brain targeting liposome and preparation method thereof
  • A kind of paeonol-ozagrel conjugate brain targeting liposome and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0094] Measure 20mL of water into a stoppered Erlenmeyer flask, put in a magnet, and preheat in a water bath at 40°C; accurately weigh 3mg of paeonol-ozagrel conjugate, 60mg of soybean lecithin, 6mg of cholesterol, DSPE-PEG 2000 5mg, DSPE-PEG 2000 Add 3mL of absolute ethanol to 1.5mg of Mal, and heat it in a water bath until it is completely dissolved to form an oil phase; inject the above drug into the preheated water slowly and uniformly with a 1mL syringe, continue to stir for 2 hours at a speed of 400r / min, and wait until the organic solvent is completely evaporated , to obtain paeonol-ozagrel conjugate long-circulating liposome suspension. 100 μL of the targeting ligand OX26 (3 mM) was thiolated according to the experimental procedure of the Traut's kit, added to the paeonol-ozagrel conjugate liposome suspension, and the coupling reaction was carried out at room temperature. After the reaction, The solution was passed through a Sepharose CL-4B column (20cm×1.5cm) to rem...

Embodiment 2

[0097] Measure 20mL of water into a stoppered Erlenmeyer flask, put in a magnet, and preheat in a water bath at 40°C; accurately weigh 4mg of paeonol-ozagrel conjugate, 60mg of soybean lecithin, 6mg of cholesterol, DSPE-PEG 2000 5mg, DSPE-PEG 2000 Add 3 mL of absolute ethanol to 2.5 mg of Mal, and heat it in a water bath until it is completely dissolved to form an oil phase; slowly and uniformly inject the above drug into the preheated water with a 1 mL syringe, continue stirring for 2 hours at a speed of 400 r / min, and wait for the organic solvent to evaporate completely , to obtain paeonol-ozagrel conjugate long-circulating liposome suspension; 100 μL targeting ligand OX26 (3mM) was thiolated according to the experimental procedure of Traut's kit, and added to paeonol-ozagrel In the Gray conjugated liposome suspension, the coupling reaction is carried out at room temperature, and the solution after the reaction is passed through a Sepharose CL-4B column (20cm×1.5cm) to remo...

Embodiment 3

[0100]Measure 20mL of water into a stoppered Erlenmeyer flask, put in a magnet, and preheat in a water bath at 40°C; accurately weigh 2mg of paeonol-ozagrel conjugate, 60mg of soybean lecithin, 6mg of cholesterol, DSPE-PEG 2000 5mg, DSPE-PEG 2000 Add 3mL of absolute ethanol to 1.5mg of Mal, and heat it in a water bath until it is completely dissolved to form an oil phase; inject the above drug into the preheated water slowly and uniformly with a 1mL syringe, continue to stir for 2 hours at a speed of 400r / min, and wait until the organic solvent is completely evaporated , to obtain paeonol-ozagrel conjugate long-circulating liposome suspension; 100 μL targeting ligand OX26 (3mM) was thiolated according to the experimental procedure of Traut's kit, and added to paeonol-ozagrel In the Gray conjugated liposome suspension, the coupling reaction is carried out at room temperature, and the solution after the reaction is passed through a Sepharose CL-4B column (20cm×1.5cm) to remove ...

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Abstract

The invention discloses a paeonol-ozagrel conjugate brain-targeted liposome and a preparation method thereof, which comprises paeonol-ozagrel conjugate, phospholipid, cholesterol, polyethylene glycol-dishard Made from fatty acylphosphatidylethanolamine, polyethylene glycol-distearoylphosphatidylethanolamine maleimide, OX26, organic solvent and water. The paeonol-ozagrel conjugate brain-targeted liposome prepared by the present invention can avoid the phagocytosis of the liver-spleen reticuloendothelial system in the drug body, and has a slow-release function, which helps to prolong the drug in vivo. Circulation time, and through the blood-brain barrier, paeonol-ozagrel conjugates can be targeted into the brain, which can better prevent or treat cardiovascular and cerebrovascular diseases caused by platelet aggregation, especially thrombotic heart disease. , Cerebral ischemia or infarction and other diseases.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a paeonol-ozagrel conjugate brain-targeting liposome and a preparation method thereof. Background technique [0002] Cardiovascular and cerebrovascular diseases are the main cause of death of the global population, with high morbidity, disability and mortality, which seriously endanger the life safety and health of patients. With the aging of the social population, the incidence is increasing day by day, effective Prevention and treatment of cardiovascular and cerebrovascular diseases are the focus of contemporary medical research. Thromboembolism is one of the important factors leading to cardiovascular and cerebrovascular diseases. Thromboembolic disease is a pathological process in which various intrinsic and extrinsic factors lead to intravascular thrombus formation and embolism, resulting in impaired tissue and organ function. Thromboembolic diseases centered on c...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/55A61K47/69A61K47/68A61K31/12A61K31/4174A61P9/00A61P9/10
CPCA61K31/12A61K31/4174A61K2300/00
Inventor 彭灿蒋苗苗佘之宝金玉陈卫东彭代银
Owner ANHUI UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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