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Co-loaded adriamycin and siRNA (small interfering ribose nucleic acid) carrier capable of removing pegylation and synthesis method thereof

A technology of PEGylation and synthesis method, which is applied in the field of co-loading doxorubicin and siRNA carrier and its synthesis, which can solve the problems of inability to play a therapeutic role, improve the drug effect, increase the effective concentration of the drug, and avoid enzymatic hydrolysis Effect

Inactive Publication Date: 2014-09-10
XI AN JIAOTONG UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the delivery of gene medicine is even more challenging because it is usually negatively charged and easily cleared by the immune system and cannot exert therapeutic effects

Method used

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  • Co-loaded adriamycin and siRNA (small interfering ribose nucleic acid) carrier capable of removing pegylation and synthesis method thereof
  • Co-loaded adriamycin and siRNA (small interfering ribose nucleic acid) carrier capable of removing pegylation and synthesis method thereof
  • Co-loaded adriamycin and siRNA (small interfering ribose nucleic acid) carrier capable of removing pegylation and synthesis method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] 1) Synthesis of cystaminated methoxypolyethylene glycol:

[0043] Dissolve dry methoxy-terminated polyethylene glycol (abbreviated as mPEG) with a molecular weight of 800Da, dibutyltin dilaurate and 2,2'-dithiodiethylisocyanate in anhydrous toluene, under nitrogen atmosphere React at 85°C for 48 hours, then precipitate in anhydrous n-hexane for 3 times, and dry the obtained solid in vacuum to obtain 2,2'-dithiodiethylisocyanate-modified mPEG; wherein, the added mPEG 1. The molar ratio of dibutyltin dilaurate to 2,2'-dithiodiethylisocyanate is 1:0.02:4, and 10g of mPEG is dissolved in every 100ml of anhydrous toluene;

[0044] Dissolve 2,2'-dithiodiethylisocyanate-modified mPEG in distilled water, then react at 60°C for 6 hours, and finally dialyze and freeze-dry the obtained reaction solution to obtain white powder cystamination Methoxy-terminated polyethylene glycol (abbreviated as cystaminated mPEG); wherein, 5 g of 2,2'-dithiodiethylisocyanate-modified mPEG was diss...

Embodiment 2

[0060] 1) Synthesis of cystaminated methoxypolyethylene glycol:

[0061] Dissolve dry methoxy-terminated polyethylene glycol (abbreviated as mPEG) with a molecular weight of 2000Da, dibutyltin dilaurate and 2,2'-dithiodiethylisocyanate in anhydrous toluene, under nitrogen atmosphere React at 85°C under a nitrogen atmosphere for 48 hours, then precipitate in anhydrous n-hexane for 3 times, and dry the obtained solid in vacuum to obtain 2,2'-dithiodiethylisocyanate-modified mPEG; wherein, the added The molar ratio of mPEG, dibutyltin dilaurate and 2,2'-dithiodiethylisocyanate is 1:0.04:4; 20g of mPEG is dissolved in 100ml of anhydrous toluene;

[0062] Dissolve 2,2'-dithiodiethylisocyanate-modified mPEG in distilled water, then react at 60°C for 6 hours, and finally dialyze and freeze-dry the obtained reaction solution to obtain white powder cystamination Methoxy-terminated polyethylene glycol (abbreviated as cystaminated mPEG); wherein, 15 g of 2,2'-dithiodiethylisocyanate-mod...

Embodiment 3

[0074] 1) Synthesis of cystaminated methoxypolyethylene glycol:

[0075] Dissolve dry methoxy-terminated polyethylene glycol (abbreviated as mPEG) with a molecular weight of 2000Da, dibutyltin dilaurate and 2,2'-dithiodiethylisocyanate in anhydrous toluene, under nitrogen atmosphere React at 85°C under a nitrogen atmosphere for 48 hours, then precipitate in anhydrous n-hexane for 3 times, and dry the obtained solid in vacuum to obtain 2,2'-dithiodiethylisocyanate-modified mPEG; wherein, the added The molar ratio of mPEG, dibutyltin dilaurate and 2,2'-dithiodiethylisocyanate is 1:0.05:5; 10g of mPEG is dissolved in 100ml of anhydrous toluene;

[0076] Dissolve 2,2'-dithiodiethylisocyanate-modified mPEG in distilled water, then react at 60°C for 6 hours, and finally dialyze and freeze-dry the obtained reaction solution to obtain white powder cystamination Methoxy-terminated polyethylene glycol (abbreviated as cystaminated mPEG); wherein, 10 g of 2,2'-dithiodiethylisocyanate-mod...

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Abstract

The invention provides a co-loaded adriamycin and siRNA (small interfering ribose nucleic acid) carrier capable of removing pegylation and a synthesis method thereof. Firstly, cystamine modification is carried out on terminated methoxyl polyethylene glycol, so that cystamine modified mPEG is obtained; then a carbodiimide method is utilized for bonding an RAFT (reversible additive fragment transfer) polymerization chain transfer agent onto the end of a cystamine modified mPEG chain, so that a macromolecule RAFT chain transfer agent; then RAFT polymerization is carried out, so that a terminated methoxyl polyethylene glycol-poly(N-(3-dimethylamine propyl) methacrylamide)-poly(N-t-butyloxycarboryl propylene hydrazide) triblock copolymer is obtained; finally a protective group (namely t-butyloxycarboryl) is removed, so that a terminated methoxyl polyethylene glycol-poly(N-(3-dimethylamine propyl) methacrylamide)-polypropylene hydrazide triblock copolymer is obtained. The synthesis method has the advantages that raw materials are available, reaction conditions are mild, molecular weight of a polymer and length of a chain of each block in the obtained carrier can be easily controlled, after adriamycin is loaded, nanoparticles can be self assembled, pharmaceutical effect is high, and co-loading of a chemotherapeutic drug and a gene-based drug is realized.

Description

technical field [0001] The invention belongs to the field of biomedical materials, and in particular relates to a depegylated co-loaded doxorubicin and siRNA carrier and a synthesis method thereof. Background technique [0002] Chemotherapy is one of the main strategies for clinical tumor treatment. It mainly uses the circulatory system to deliver cytotoxic chemical drugs to the diseased site, and at the same time inevitably brings toxic side effects to normal cells in the body. The curative effect and toxic and side effects of chemotherapy drugs are closely related to the dosage. Therefore, how to improve the efficacy of chemotherapy drugs and avoid their side effects is always the most concerned issue in cancer chemotherapy. At present, the development of molecularly targeted drugs and drug delivery systems has become a research hotspot. Among them, the development of molecularly targeted drugs is relatively slow due to problems such as development difficulties and clini...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/48A61K9/51A61K48/00A61K31/704A61P35/00
Inventor 姚煜钱军民徐明辉胥伟军
Owner XI AN JIAOTONG UNIV
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