Nanoparticles of Disulfiram Loaded on Polyester Materials and Its Application, Pharmaceutical Preparations and Its Application

A technology for pharmaceutical preparations and nanoparticles, which can be applied to medical preparations without active ingredients, medical preparations containing active ingredients, and drug combinations, etc., which can solve the problems of low loading efficiency, few successful reports, and leakage of nanoparticles. drug and other problems, to achieve the effect of effective loading and ensuring drug stability

Active Publication Date: 2018-10-16
CHANGCHUN INST OF APPLIED CHEMISTRY - CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the special molecular structure of disulfiram, the loading efficiency of the usual amphiphilic nanomicelles is very low; due to the compatibility problem, the drug leakage phenomenon of the prepared nanoparticles is also very serious. Little effect on improving the stability of disulfiram
Therefore, although disulfiram has shown great potential in tumor therapy in vitro, there are very few successful reports of disulfiram in vivo in open literature.
The reason is that, so far, there is no effective and stable method for carrying disulfiram at home and abroad.

Method used

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  • Nanoparticles of Disulfiram Loaded on Polyester Materials and Its Application, Pharmaceutical Preparations and Its Application
  • Nanoparticles of Disulfiram Loaded on Polyester Materials and Its Application, Pharmaceutical Preparations and Its Application
  • Nanoparticles of Disulfiram Loaded on Polyester Materials and Its Application, Pharmaceutical Preparations and Its Application

Examples

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preparation example Construction

[0043] The preparation of the disulfiram nanoparticles described in this application can be prepared by the nanoprecipitation method or the thin film emulsification method, specifically:

[0044] Mix disulfiram or its derivatives, polyethylene glycol-polyester block copolymer, polycaprolactone and solvent, then mix with water for injection, stir, dialyze the organic solvent and filter to obtain disulfiram nanoparticles Solution.

[0045] Or use the following method to prepare the disulfiram composition:

[0046] The solution of disulfiram nanoparticles obtained above is mixed with trehalose and freeze-dried to obtain a freeze-dried powder of disulfiram nanoparticles.

[0047] The disulfiram composition of the present application preferably has a particle size of 20 to 200 nm, and it is a solution or dry powder.

[0048] The disulfiram nanoparticles provided by the present invention propose to use the mixed material of polyethylene glycol-polyester block copolymer and poly-caprolactone ...

Embodiment 1

[0054] Example 1 Preparation of disulfiram nanoparticles

[0055] Take 1.0g of disulfiram, polyethylene glycol-polyglycolide block copolymer (number average molecular weight: polyethylene glycol 5000Da, polyglycolide 2000Da) 3.0g, polycaprolactone (number average molecular weight) : 3400Da) 6.0g, dissolved in 500mL of a mixed solvent of acetonitrile and DMF (v / v=1 / 1), and then added dropwise to 2.0L of water for injection with stirring. After the dripping is completed, the stirring is continued for 2 hours, and then the organic solvent is dialyzed off, filtered, and the solution of disulfiram nanoparticles is collected. Such as image 3 As shown, image 3 This is a transmission electron micrograph of the disulfiram nanoparticles prepared in this example.

Embodiment 2

[0056] Example 2 Preparation of freeze-dried disulfiram nanoparticles

[0057] The disulfiram nanoparticle solution prepared in Example 1 is mixed with trehalose (the mass of which is the volume of the disulfiram nanoparticle solution×5%), and freeze-dried to obtain a freeze-dried powder of disulfiram nanoparticles.

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Abstract

The invention provides nanoparticles of disulfiram loaded on polyester materials, which are prepared from the following components: 1-20 parts by weight of disulfiram or its derivatives, polyethylene glycol-polyester block copolymer 20 to 95 parts by weight, and 5 to 80 parts by weight of polycaprolactone. The disulfiram nanoparticles designed by the present invention provide a hydrophobic inner core by polycaprolactone, stably encapsulate disulfiram inside, and the polyethylene glycol-polyester block copolymer is modified on the surface to ensure the stability of the disulfiram nanoparticles. Solubility and long cycle ability. The application also provides the application of the disulfiram nanoparticles in treating tumors.

Description

Technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to a polyester material-supported disulfiram nanoparticle and its application, pharmaceutical preparation and its application. Background technique [0002] Disulfiram (disulfiram, DSF), also known as tetraethylthiuram disulfide or disulfiram, its structure is shown in formula I. Since disulfiram was first synthesized in 1881, it has been used as a catalyst for rubber vulcanization in the rubber industry. In 1948, Jacobsen and others in Copenhagen found that disulfiram can cause facial flushing, headache, abdominal pain, sweating, palpitations, and dyspnea after being absorbed by humans in a small amount. The symptoms are more obvious after taking the drug. The performance is named "disulfiram-like reaction". The mechanism of disulfiram causing this reaction is that it can inhibit the acetaldehyde dehydrogenase (ALDH) in the liver, so that after ethanol is oxidized ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/14A61K31/145A61K47/34A61P35/00
Inventor 汤朝晖宋万通于海洋张瑜陈学思
Owner CHANGCHUN INST OF APPLIED CHEMISTRY - CHINESE ACAD OF SCI
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