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Oxidized-graphene nano-drug carrier with targeting function and preparing method thereof

A nano-drug carrier, graphene technology, applied in the field of medicine, can solve the problems of low drug loading, large toxic and side effects, etc.

Inactive Publication Date: 2017-05-24
CHANGZHOU IND TECH RES INST OF ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The first purpose of the present invention is to solve the defects of low drug loading and high toxic and side effects of anti-tumor targeted drugs in the prior art, and provide a drug with low toxic and side effects, long circulation time in the blood, and the ability to target Nanoscale drug carriers for action and responsive drug release

Method used

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  • Oxidized-graphene nano-drug carrier with targeting function and preparing method thereof
  • Oxidized-graphene nano-drug carrier with targeting function and preparing method thereof
  • Oxidized-graphene nano-drug carrier with targeting function and preparing method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Polyethylene glycol NH with a molecular weight of 3000 2 -PEG-NH 2 Add 1-pyrenebutyric acid to the organic solvent DMF in a molar ratio of 1:0.5, the amount of DMF is 30 times the mass of the reactant, and react at 100°C for 6 hours. After the reaction, the mixed solution is dialyzed and freeze-dried You can get PyBA-PEG-NH 2 ; then PyBA-PEG-NH 2 Add folic acid to DMSO at a molar ratio of 1:2, react at 100°C for a period of 8 hours, dialyze the mixed solution after the reaction and freeze-dry to obtain PyBA-PEG-FA;

[0028] Then cystamine and 1-pyrenebutyric acid were added to the organic solvent DMSO at a molar ratio of 1:0.3, and reacted for a period of 12 hours at room temperature. After the reaction was completed, the mixed solution was dialyzed and freeze-dried to obtain PyBA-S-S-NH 2 ; then PyBA-S-S-NH 2 Treat it with succinic anhydride to form PyBA-S-S-COOH and add the antitumor drug DOX into the organic solvent dioxane at a molar ratio of 1:4, react at room ...

Embodiment 2

[0034] Polyethylene glycol NH with a molecular weight of 4000 2 -PEG-NH 2 Add 1-pyrenebutyric acid to the organic solvent DMSO at a molar ratio of 1:1, the amount of DMSO is 10 times the mass of the reactant, and react at 100°C for 8 hours. After the reaction is completed, the mixed solution is dialyzed and freeze-dried You can get PyBA-PEG-NH 2 ; then PyBA-PEG-NH 2 Add folic acid to DMF at a molar ratio of 1:3, react at 100°C for a period of 12 hours, dialyze the mixed solution after the reaction and freeze-dry to obtain PyBA-PEG-FA;

[0035] Then cystamine and 1-pyrenebutyric acid were added to the organic solvent DMSO at a molar ratio of 1:0.6, and reacted for a period of 18 hours at room temperature. After the reaction was completed, the mixed solution was dialyzed and freeze-dried to obtain PyBA-S-S-NH 2 ; then PyBA-S-S-NH 2 Treat it with succinic anhydride to form PyBA-S-S-COOH and add the antineoplastic drug DOX to the organic solvent dioxane at a molar ratio of 1:3...

Embodiment 3

[0041] Polyethylene glycol NH2-PEG-NH with a molecular weight of 5000 2 Add 1-pyrenebutyric acid to the organic solvent DMF at a molar ratio of 1:0.5, and react at 80°C for 12 hours. After the reaction is completed, dialyze the mixed solution and freeze-dry to obtain PyBA-PEG-NH 2 ; then PyBA-PEG-NH 2 Add folic acid to DMF at a molar ratio of 1:5, react at 100°C for 6 hours, dialyze the mixed solution after the reaction and freeze-dry to obtain PyBA-PEG-FA;

[0042] Then cystamine and 1-pyrenebutyric acid were added to the organic solvent DMSO at a molar ratio of 1:1, and reacted at room temperature for 24 hours. After the reaction was completed, the mixed solution was dialyzed and freeze-dried to obtain PyBA-S-S-NH 2 ; then PyBA-S-S-NH 2 Treat it with succinic anhydride to form PyBA-S-S-COOH and add the antineoplastic drug DOX into the organic solvent dioxane at a molar ratio of 1:5, react at room temperature for 12 hours, dialyze the mixed solution after the reaction, and ...

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Abstract

The invention relates to an oxidized-graphene nano-drug carrier with a targeting function. The oxidized-graphene nano-drug carrier comprises oxidized-graphene, PyBA PEG FA and PyBA S S Drug. The invention further provides a preparing method of the oxidized-graphene nano-drug carrier, and the preparing method comprises the steps of firstly using polyethylene glycol with dual-amidogens be subjected to coupled reactions with folic acid and pyrene-1-butyric acid respectively to prepare PyBA PEG FA, conducting a reaction among pyrene-1-butyric acid and cystine and adriamycin amycin to prepare PyBA S S Drug, then mixing oxidized-graphene, PyBA PEG FA and PyBA S S Drug according to a certain proportion, conducting stirring and time treatment to some degree to obtain a nano-drug carrier solution with a certain concentration. The preparing method of the oxidized-graphene nano-drug carrier is simple in technology, and the obtained nano-drug carrier has high drug-carrying efficiency, and has a redox-responsive property and targeting property; meanwhile, various kinds of materials used for preparing the carrier have good biocompatibility.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a graphene oxide-based nano drug carrier with targeting effect and a preparation method thereof. Background technique [0002] With the increasing development of nanotechnology and biopharmaceuticals, nano drug carriers have become a hot research field. Nano-drug carriers can efficiently load drugs, deliver targeted drugs and release drugs in a controlled manner. And it can prolong the action time of the medicine, and has the advantages of biocompatibility, small toxic and side effects, and the like. Nano-drug carriers can be divided into nanoparticles, nano-liposomes, polymer gels and nano-magnetic particles. Common nano-drug carriers include carbon nanotubes, microspheres, liposomes, or ferrite magnetic particles, which load drugs through surface adsorption, hydrogen bonding, intercalation, or other reactions. [0003] Graphene is a new type of nanomaterial with two-dimensional honey...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/04A61K47/54A61K47/22A61K45/00A61P35/00
CPCA61K47/02A61K45/00A61K47/22
Inventor 魏伟潘祥华
Owner CHANGZHOU IND TECH RES INST OF ZHEJIANG UNIV
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