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Hydrogen peroxide-responsive targeted drug-loaded nanomaterial and preparation method

A drug-loaded nano-hydrogen peroxide technology, applied in the field of nano-materials, can solve problems such as the lack of application of nano-drug-loaded systems, and achieve the effect of improving drug availability

Inactive Publication Date: 2020-09-15
JILIN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, in the field of atherosclerotic diseases, the application of nano-drug delivery system integrating diagnosis and treatment is relatively lacking, which needs to be supplemented and improved urgently.

Method used

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  • Hydrogen peroxide-responsive targeted drug-loaded nanomaterial and preparation method
  • Hydrogen peroxide-responsive targeted drug-loaded nanomaterial and preparation method
  • Hydrogen peroxide-responsive targeted drug-loaded nanomaterial and preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Embodiment 1: the synthesis of polyhydroxyethyl methacrylate (PHEMA)

[0025] Poly(hydroxyethylmethacrylate) (PHEMA) was synthesized by ATRP method. 2-Bipyridine (0.06g), CuCl (0.28g), 4mL N,N'-dimethylformamide, 4mL formamide were successively added to a branched bottle that was baked several times, vacuumed, and filled with argon. hydroxyethyl acrylate and 0.15 mL 2-bromo-2 methacrylate. Carry out vacuum pumping and argon filling operation again to ensure that the reaction system is in an oxygen-free state. Place the check bottle in an oil bath at 70°C for 6 hours. After the reaction is terminated, dissolve the mixture in methanol and use Al 2 o 3 The neutral column removes impurities, and the filtrate is concentrated by rotary evaporation, and precipitated in ether, and then centrifuged, dried and other post-treatments to obtain white powder PHEMA.

Embodiment 2

[0026] Example 2: Synthesis of Hydrogen Peroxide Responsive Simvastatin Polymer (PHEMA-Sim)

[0027] First, simvastatin (1.72g) was dissolved in 20mL of anhydrous dichloromethane, and oxalyl chloride (5.02g) was dissolved in 5mL of anhydrous dichloromethane. Under the condition of ice-salt bath, drop the simvastatin solution into the oxalyl chloride solution at a rate of 1 drop per second, continue to react for 2 hours after the addition, the reaction solution gradually changes from colorless to yellow, and the reaction ends. Subsequently, the solvent and excess oxalyl chloride were removed by rotary evaporation, and 1.84 g of simvastatin acid chloride yellow powder was obtained after vacuum drying, which was re-dissolved in 20 mL of anhydrous dichloromethane. Afterwards, the PHEMA (0.9g) prepared in Example 1 was dissolved in 50mL of anhydrous dichloromethane, and under the protection of argon, the dichloromethane solution containing simvastatin acyl chloride was dropped at a...

Embodiment 3

[0028] Example 3: Synthesis of targeted drug-loaded nanoparticles (PHEMA-Sim-ISO-1) in response to hydrogen peroxide

[0029] PHEAM-Sim (0.92g), ISO-1 (0.44g) and DMAP (0.12g) prepared in Example 2 were dissolved in 30mL of dichloromethane, and DCC (0.4g) was dissolved in 4mL of dichloromethane, Drop into the former mixed solution at a rate of 1 drop per second. After the dropwise addition, the reaction was continued for 24 h at room temperature. After the reaction, the target product PHEMA-Sim-ISO-1 was obtained by filtration, dialysis and drying. NMR image such as figure 1 shown, from figure 1 It can be seen that each H position and peak area of ​​the target product have a good assignment. Transmission scanning electron microscope such as figure 2 shown, from figure 2 It can be seen that the product can form a spherical structure with a particle size of about 50 nm.

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Abstract

The invention discloses a hydrogen peroxide response-type targeted medicine carrying nanomaterial and a preparation method, and belongs to the technical field of nanomaterials. The structural formulaof the hydrogen peroxide response-type targeted medicine carrying nanomaterial is shown in the description. The preparation method comprises synthesis of PHEMA (Polyhydroxyethyl Methacrylate), synthesis of PHEMA-Sim / Prv / Com / Lo and synthesis of PHEMA-Sim / Prv / Com / Lo-ISO-1. Nanoparticles prepared by the method have high medicinal utilization rate, and a function of targeting atherosclerotic plaques.

Description

technical field [0001] The invention belongs to the technical field of nanometer materials, and in particular relates to a nanometer drug-loaded material with hydrogen peroxide response and targeting functions and a preparation method thereof. Background technique [0002] Poly(hydroxyethyl methacrylate) is easy to modify due to its unique polyhydroxy structure, and has certain applications in the medical field. However, the use of polyhydroxyethyl methacrylate to carry drugs and target molecules at the same time, as a carrier for both diagnosis and treatment is not common. [0003] Atherosclerosis is a common cardiovascular and cerebrovascular disease. As a chronic inflammatory disease, atherosclerosis is latent and hidden in the early stage, and the symptoms are not obvious, but it can eventually lead to high-risk diseases such as myocardial infarction and stroke. In terms of treatment, atherosclerotic disease can only be cured by stents, surgery and other means in the la...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C08F8/30C08F8/14C08F220/20C08F220/22A61K9/107A61K47/32A61K47/22A61K47/58A61K31/366A61P9/10
CPCA61K9/1075A61K31/366A61K47/22A61K47/32A61K47/58A61P9/10C08F8/30C08F220/20C08F8/14C08F220/22
Inventor 李亚鹏方超赵外欧王书唯
Owner JILIN UNIV
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