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Polydopamine nanocarrier delivery system for targeted activation of CD44 molecule, and preparation method and application thereof

A dopamine nanometer and nanocarrier technology, which can be applied to preparations for in vivo experiments, nanotechnology, nanotechnology, etc., can solve the problems of limited application of drug carriers, cumbersome steps, and low drug load.

Active Publication Date: 2021-01-29
BEIJING INNO MEDICINE CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, the following problems will be encountered in the research and development of targeted drug delivery systems targeting CD44: if the affinity between CD44 and HA on the surface of target cells is not enough to provide significant specificity, then such targeted drug delivery systems will be difficult to obtain. There will be no specific targeting properties
The disadvantage of this method is that the strategy of passively adsorbing drugs into the carrier has low drug loading and cumbersome steps, which limit its application as a drug carrier.

Method used

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  • Polydopamine nanocarrier delivery system for targeted activation of CD44 molecule, and preparation method and application thereof
  • Polydopamine nanocarrier delivery system for targeted activation of CD44 molecule, and preparation method and application thereof
  • Polydopamine nanocarrier delivery system for targeted activation of CD44 molecule, and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0147] Copolymerized nanocarriers formed by different ratios of tannic acid and dopamine in embodiment 1

[0148] Mix 20mL of ultrapure water, 5mL of ethanol, and 1mL of ammonia water evenly, continue heating until the water temperature reaches and maintains at 50°C, weigh a certain amount of dopamine hydrochloride (molecular weight 189.64) and 0.1 g of tannic acid (molecular weight 1701) and evenly disperse in a small amount of Ultrapure water was added dropwise to the above solution. React at room temperature in the dark for 24 hours, purify the above-mentioned nanocarriers by ultrafiltration, and freeze-dry to obtain different PDA / TA blends of brown-black products. figure 1 The infrared spectra of PDA and the mixed polymerization of PDA and TA to obtain nanocarriers are shown.

Embodiment 2

[0149] Example 2 Loading Rosuvastatin (R) Nanocarriers of Polydopamine (PDA) Surface-Modified Hyaluronic Acid (HA) Preparation of PDA(R)-HA

[0150] 2.1. Preparation of blank polydopamine (PDA) nanocarriers

[0151] Mix 20mL of ultrapure water, 5mL of ethanol, and 1mL of ammonia water evenly, continue heating until the water temperature reaches and maintains at 50°C, weigh 0.1g of dopamine hydrochloride and evenly disperse it in a little ultrapure water, and add it dropwise to the above solution at room temperature. After 24 hours of light reaction, the nanocarrier was purified by ultrafiltration, and freeze-dried to obtain the brown-black product PDA.

[0152] 2.2 Preparation of polydopamine (PDA) nanocarriers loaded with rosuvastatin (R) Mix 20mL ultrapure water, 5mL ethanol, and 1mL ammonia water evenly, continue heating until the water temperature reaches and maintains at 50°C, and weigh 0.1g of Dopamine hydrochloride was uniformly dispersed in a little ultrapure water,...

Embodiment 3

[0154] Embodiment 3 Coupling polyethylene glycol, selectin (SP) simultaneously, loading rosuvastatin (R) polydopamine (PDA) sodium Preparation of rice carrier (PDA(R)-PEG / SP)

[0155] 3.1 Preparation of rosuvastatin-loaded polydopamine nanocarriers (PDA(R)-PEG) coupled with polyethylene glycol

[0156] Mix 20mL of ultrapure water, 5mL of ethanol, and 1mL of ammonia water evenly, continue heating until the water temperature reaches and maintains at 50°C, weigh 0.1g of dopamine hydrochloride and evenly disperse it in a little ultrapure water, and add it dropwise to the above solution , after stirring at 50°C for 1h, 5ml 1.0mg mL -1 The DMSO solution of rosuvastatin was added dropwise to the above polymerization solution, and after reacting in the dark at room temperature for 24 hours, amino-modified polyethylene glycol (PEG-NH 2 ) aqueous solution (1.0mL, 1.0mg mL -1 ), continue to stir and react for 4 hours. The above nanocarriers were purified by ultrafiltration and fre...

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Abstract

The present invention provides a polydopamine nanocarrier delivery system for targeted activation of a CD44 molecule. According to the invention, the surface of a polydopamine nanocarrier is partiallymodified with a targeting ligand, and the targeting ligand is a ligand capable of specifically binding to the activated CD44 molecule. According to the nanocarrier and a preparation method thereof, the method is simple in process, and the nanocarrier is high in drug loading capacity, high in yield, good in adaptability to various drugs and convenient to couple with various targeting ligands. Meanwhile, the nanocarrier is endowed with a good drug sustained release function in the preparation process. The invention provides a simple method capable of realizing simultaneous synthesis and drug loading of the polydopamine nano-drug carrier through a one-pot process, wherein a drug loading procedure and the procedure of polymerizing dopamine to form the nanoparticle drug carrier are completed in one step. The method is simple, convenient, green and controllable; and the nanocarrier is high in drug loading capacity, good in compatibility with various drugs, good in biocompatibility, high insafety and easy for targeted ligand modification.

Description

technical field [0001] The invention belongs to the technical field of targeted drug delivery, and in particular relates to a natural polydopamine macromolecule nanocarrier for targeting and activating CD44 molecules, especially targeting vulnerable plaques. The present invention also relates to the innovative preparation of said nanocarriers, especially the preparation and use of polydopa nano-delivery systems, especially in the diagnosis, prevention and treatment of vulnerable plaques or diseases associated with vulnerable plaques the use of. Background technique [0002] At present, acute cardiovascular events, mainly acute myocardial infarction and sudden cardiac death, have become the number one killer of human health. According to statistics, about 20 million people die of acute cardiovascular events in the world every year. In China, the situation is also not optimistic. More than 700,000 people die of acute myocardial infarction and sudden cardiac death every year,...

Claims

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Application Information

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IPC IPC(8): A61K47/69A61K47/34A61K47/60A61K47/61A61K47/62A61K47/68A61K45/00A61K49/00A61K49/04A61K49/18A61K51/12B82Y5/00A61P9/10A61P9/00A61P35/00A61P9/04
CPCA61K47/6935A61K47/61B82Y5/00A61K47/68A61K47/62A61K47/60A61K45/00A61K49/0002A61K49/0485A61K49/1824A61K51/1244A61P9/10A61P9/00A61P35/00A61P9/04
Inventor 马茜孙洁芳
Owner BEIJING INNO MEDICINE CO LTD
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