Heat-sensitive drug-loaded nano particle based on conjugated polymer and preparation method of heat-sensitive drug-loaded nano particle

A technology of conjugated polymers and drug-loaded nanometers, which can be used in pharmaceutical formulations, preparations for in vivo tests, and medical preparations with non-active ingredients. To overcome the limited specificity of cancer cells and other issues, achieve good biocompatibility, effective and controllable drug release, and shorten the particle distance

Inactive Publication Date: 2019-06-28
SHAANXI NORMAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] Cancer has always been one of the major threats to human life. In addition to surgical intervention, the current treatment methods for cancer mainly rely on chemotherapy and radiotherapy. In many cases, surgery cannot completely remove all cancer cells in the human body, and chemotherapy and radiotherapy are due to The specificity of cancer cells is limited, while killing cancer cells, it will cause serious toxic side effects to healthy tissues and organs, which greatly affects the therapeutic effect

Method used

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  • Heat-sensitive drug-loaded nano particle based on conjugated polymer and preparation method of heat-sensitive drug-loaded nano particle
  • Heat-sensitive drug-loaded nano particle based on conjugated polymer and preparation method of heat-sensitive drug-loaded nano particle
  • Heat-sensitive drug-loaded nano particle based on conjugated polymer and preparation method of heat-sensitive drug-loaded nano particle

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031]

[0032] 1. Under nitrogen, add 66.24mg (0.1mmol) formula I-1 compound, 18.72mg (0.08mmol) p-diiodobenzene, 10.78mg (0.02mmol) formula III-1 compound, 1.0 mL dimethylformamide, 0.5mL triethylamine, 1.12mg (0.005mmol) palladium acetate, 6.94mg (0.023mmol) tri-p-cresyl phosphate, stirred and reacted at 90°C for 24h, cooled to room temperature, and dialyzed , freeze-drying to obtain conjugated polymer 1. As tested by gel permeation chromatography, Mn=16600, Mw=18816 and PDI=1.13 of the conjugated polymer 1.

[0033] 2. Dissolve 0.1 mg of conjugated polymer 1, 0.025 mg of PNIPAM with a number average molecular weight of 20,000 to 40,000, and 0.05 mg of doxorubicin in 5 mL of methanol, and quickly pour the resulting solution into a container containing In a flask of 20mL ultrapure water, sonicate for 20min. After the ultrasonication was completed, return to room temperature, use a needle to blow nitrogen and heat to remove methanol and part of the ultrapure water in the...

Embodiment 2

[0035] 1. Prepare conjugated polymer 1 according to the method in step 1 of Example 1.

[0036] 2. Dissolve 0.1 mg of conjugated polymer 1, 0.05 mg of PNIPAM with a number average molecular weight of 20,000 to 40,000, and 0.05 mg of doxorubicin in 5 mL of methanol, and quickly pour the resulting solution into a container containing In a flask of 20mL ultrapure water, sonicate for 20min. After the ultrasonication was completed, return to room temperature, use a needle to blow nitrogen and heat to remove methanol and part of the ultrapure water in the mixed solution, and concentrate the solution to 5 mL to obtain thermosensitive doxorubicin-loaded nanoparticles based on conjugated polymers.

Embodiment 3

[0038] 1. Prepare conjugated polymer 1 according to the method in step 1 of Example 1.

[0039]2. Dissolve 0.1 mg of conjugated polymer 1, 0.015 mg of PNIPAM with a number average molecular weight of 20,000 to 40,000, and 0.05 mg of doxorubicin in 5 mL of methanol, and quickly pour the resulting solution into a container containing In a flask of 20mL ultrapure water, sonicate for 20min. After the sonication is completed, return to room temperature, use a needle to blow nitrogen and heat to remove methanol and part of the ultrapure water in the mixed solution, and concentrate the solution to 5 mL, based on conjugated polymer thermosensitive doxorubicin-loaded nanoparticles.

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Abstract

The invention discloses a heat-sensitive drug-loaded nano particle based on a conjugated polymer and a preparation method of the heat-sensitive drug-loaded nano particle. The nano particle is a nanoball taking the conjugated polymer coated with an antitumor drug as the core and taking a heat-sensitive polymer as the shell and formed by the conjugated polymer coated with the antitumor drug and theheat-sensitive polymer through hydrophobic interaction. The heat-sensitive drug-loaded nano particle based on the conjugated polymer has the advantages that the biocompatibility and photostability aregood, effective and controllable drug release can be achieved, and a large amount of active oxygen can be generated under the irradiation of white light, so that the synergistic treatment of photodynamic therapy can also be performed while the drug is released; in addition, since the heat-sensitive drug-loaded nano particle has excellent fluorescence properties, the heat-sensitive drug-loaded nano particle can also be used for cell imaging and drug release tracking.

Description

technical field [0001] The invention belongs to the technical field of drug delivery, and in particular relates to a class of thermosensitive drug-loaded nanoparticles based on conjugated polymers and a preparation method of the nanoparticles. Background technique [0002] Cancer has always been one of the major threats to human life. In addition to surgical intervention, the current treatment methods for cancer mainly rely on chemotherapy and radiotherapy. In many cases, surgery cannot completely remove all cancer cells in the human body, and chemotherapy and radiotherapy are due to The specificity to cancer cells is limited, while killing cancer cells, it will cause serious toxic side effects to healthy tissues and organs, which greatly affects the therapeutic effect. Therefore, it is urgent to develop more efficient therapies that can overcome physiological barriers, distinguish between malignant and benign cells, selectively target cancerous tissues, intelligently respon...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/51A61K47/32A61K31/704A61K41/00A61K49/00A61P35/00C08G61/12G01N21/64
Inventor 唐艳丽卢转宁
Owner SHAANXI NORMAL UNIV
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