Disulfiram-based glucan nanometer prodrug, and preparation method and application thereof

A nano-drug, dextran technology, applied in the field of polymers, can solve the problems of limiting the clinical application of disulfiram, fast metabolism, poor stability, etc., and achieve the effects of low cost, good hydrophilicity, and good biocompatibility

Active Publication Date: 2020-12-25
SHANGHAI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although disulfiram has excellent anticancer efficacy, it has poor stability, low solubility, fast metabolism, and is easily eliminated in blood circulation
These factors limit the clinical application of disulfiram

Method used

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  • Disulfiram-based glucan nanometer prodrug, and preparation method and application thereof
  • Disulfiram-based glucan nanometer prodrug, and preparation method and application thereof
  • Disulfiram-based glucan nanometer prodrug, and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] In this example, see figure 1 and image 3 , a method for preparing disulfiram-based dextran nano drug prodrugs, the steps are as follows:

[0035] (1) Preparation of side chain hydroxylated dextran:

[0036] Weigh 1g of dextran and 200mg of LiCl into a 100mL three-necked flask and place it in a vacuum drying oven, set the temperature at 75°C, and dry under vacuum for 72h; after the drying, add 10mL of anhydrous N , in N-dimethylformamide (DMF) and set the temperature of the oil bath to 90°C and stir until the liquid is clear; remove the oil bath after the liquid is clear, place it in an ice bath after standing to cool, and slowly and continuously pass nitrogen protection, Then add 0.59 mL of pyridine, so that the amount of pyridine is twice the molar amount of phenyl p-nitrochloroformate, then add 0.75 mg of phenyl p-nitrochloroformate in batches, and react under ice bath conditions (0°C) for 24 hours; The amount of phenyl p-nitrochloroformate is calculated based on...

Embodiment 2

[0053] This embodiment is basically the same as Embodiment 1, especially in that:

[0054] In this example, see figure 1 and image 3 , a method for preparing disulfiram-based dextran nano drug prodrugs, the steps are as follows:

[0055] (1) Preparation of side chain hydroxylated dextran:

[0056] Weigh 5g of dextran and 200mg of LiCl into a 100mL three-necked flask and place it in a vacuum drying oven, set the temperature at 75°C, and dry it under vacuum for 72h; after the drying, add 10mL of anhydrous N , in N-dimethylformamide (DMF) and set the temperature of the oil bath to 90°C and stir until the liquid is clear; remove the oil bath after the liquid is clear, place it in an ice bath after standing to cool, and slowly and continuously pass nitrogen protection, Subsequently, 1.18 mL of pyridine was added, so that the amount of pyridine was twice the molar amount of phenyl p-nitrochloroformate, and then 1.5 mg of phenyl p-nitrochloroformate was added in batches, and the ...

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Abstract

The invention discloses a disulfiram-based glucan nanometer prodrug, and a preparation method and applications thereof. The disulfiram-based glucan nanometer prodrug is a disulfiram-based glucan nanometer prodrug with oxidation-reduction response characteristics, glucan is selected as a skeleton, and a drug is connected with a polymer skeleton through a disulfide bond. The invention provides a polymer drug delivery system with oxidation-reduction response. According to the nanometer prodrug, the disulfide bond can be reduced into sulfydryl by reduced glutathione in cancer cells, and a responsemechanism is provided, so that the structure of a carrier is changed, and the drug is quickly released. The nanometer prodrug shows good biological safety and a good cancer cell killing effect, and an intelligent drug delivery system is provided for tumor treatment.

Description

technical field [0001] The present invention relates to the technical field of polymers, more specifically to a method for preparing a redox-responsive dextran-based nano-prodrug, and more specifically to a chemical modification based on thiolated dextran, Preparation of disulfide-linked dextran-diethyldithiocarbamate for application in smart drug delivery systems. Background technique [0002] Nanoscale drug precursors have been extensively studied in the field of cancer chemotherapy. Nano drug prodrugs are generally divided into carrier nano drug prodrugs and bionano drug prodrugs. The carrier nano-drug prodrug mainly connects the active compound to the carrier through a covalent bond, and after a certain reaction in the body, the active compound falls off and exerts pharmacological activities. Dextran, a natural polysaccharide, is widely used in the preparation of nano-drug prodrugs due to its excellent biocompatibility. [0003] Disulfiram (DSF), a member of the dithi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/61A61K47/69A61K31/145A61P35/00C08B37/02
CPCA61K47/61A61K47/6939A61K31/145A61P35/00C08B37/0009
Inventor 金荣余诚云孙靖王敏强曹傲能
Owner SHANGHAI UNIV
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