Mitochondrion-targeting photothermal therapeutic agent as well as preparation and application thereof

A photothermal therapy agent and mitochondrial technology, which can be used in the photo-splitting of drugs in the body, medical preparations with non-active ingredients, and medical preparations containing active ingredients, etc. Controlled gas release and other issues, to achieve high-efficiency anti-tumor therapy, simple synthesis steps, and enhanced therapeutic effects.

Inactive Publication Date: 2020-09-22
NANTONG UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, due to the fast and free diffusion behavior of NO gas molecules, it is difficult for both drug delivery methods to achieve targeted gas delivery and controllable gas release.

Method used

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  • Mitochondrion-targeting photothermal therapeutic agent as well as preparation and application thereof
  • Mitochondrion-targeting photothermal therapeutic agent as well as preparation and application thereof
  • Mitochondrion-targeting photothermal therapeutic agent as well as preparation and application thereof

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preparation example Construction

[0029] The preparation method of the above-mentioned photothermal therapeutic agent comprises the following steps:

[0030] In step 1, a CuS nanodisk is synthesized by a high-temperature solvothermal preparation method.

[0031] Add 65mg of copper acetylacetonate, 30mL of 1-octadecene and 30mL of oleylamine into a 250mL three-necked flask with a magnetic stirring rate of 350r / min, and heat at a rate of 3°C / min to 150°C and stabilize for 30min. Another weighed 7.95mg of sublimed sulfur powder was dissolved in 5mL of oleylamine, heated to 150°C under the protection of argon, and stabilized for 10min. The sulfur-dissolved oleylamine solution was quickly injected into the previous 1-octadecene solution, and the reaction was continued for 1 h. After the reaction was completed, protected by argon, cooled naturally to room temperature, 20 mL of acetone solution was added to precipitate the product, collected by centrifugation, and washed three times with absolute ethanol to remove ...

Embodiment 1

[0052] (1) Preparation of CuS nanodisks.

[0053] Add 65mg of copper acetylacetonate, 30mL of 1-octadecene and 30mL of oleylamine into a 250mL three-necked flask with a magnetic stirring rate of 350r / min, and heat at a rate of 3°C / min to 150°C and stabilize for 30min. Another weighed 7.95mg of sublimed sulfur powder was dissolved in 5mL of oleylamine, heated to 150°C under the protection of argon, and stabilized for 10min. The sulfur-dissolved oleylamine solution was quickly injected into the previous 1-octadecene solution, and the reaction was continued for 1 h. After the reaction was completed, protected by argon, cooled naturally to room temperature, 20 mL of acetone solution was added to precipitate the product, collected by centrifugation, and washed three times with absolute ethanol to remove oleylamine and 1-octadecene. The final product obtained was dispersed in 10 mL of diethylene glycol.

[0054] (2) Preparation of PEI-modified CuS nanodisks (CuS-PEI).

[0055] W...

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Abstract

The invention discloses a mitochondrion-targeting photothermal therapeutic agent as well as preparation and application thereof and belongs to the technical field of pharmaceutical preparations. The photothermal therapeutic agent comprises copper sulfide nanoparticles, the surfaces of the copper sulfide nanoparticles are modified with polyethyleneimine and (4-carboxybutyl)triphenylphosphonium bromide, the surfaces of the copper sulfide nanoparticles are modified with polyethyleneimine through ligand exchange, and the (4-carboxybutyl)triphenylphosphonium bromide is connected to the surfaces ofthe copper sulfide nanoparticles through amido bonds; secondary amine in the polyethyleneimine molecules and nitric oxide gas molecules are subjected to high-pressure electrophilic addition to form nitric oxide gas release molecule azo diol alkene salt. The NO release molecule can release NO gas under near-infrared irradiation, gas treatment is achieved, the treatment effect is further enhanced incombination with photothermal treatment of a therapeutic agent, and more efficient anti-tumor treatment is achieved.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a mitochondria-targeted photothermal therapeutic agent and its preparation and application. Background technique [0002] Cancer is one of the deadliest diseases in the world. According to the global cancer report released by the World Health Organization, about 9.6 million people died of various cancers in the world in 2018. Traditional tumor treatment methods include: surgery, radiotherapy, chemotherapy, etc., but these traditional treatment methods usually cause damage to healthy cells and cause toxic side effects to the human body. Especially in chemotherapy, anticancer drugs are usually difficult to reach the tumor site completely, so it has caused great damage to normal tissues and cells. Moreover, due to the extensive use of anticancer drugs, tumor cells have developed drug resistance The therapeutic effect of chemotherapy is greatly reduc...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K41/00A61K33/00A61K47/52A61K47/54A61K47/59A61K47/69A61P35/00
CPCA61K41/0052A61K33/00A61K41/0042A61K47/52A61K47/542A61K47/59A61K47/6935A61P35/00
Inventor 汪洋姚勇王丹琪
Owner NANTONG UNIVERSITY
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