Preparation method of multi-stimulation-response cooperative anti-tumor polymer prodrug

An anti-tumor and polymer technology, applied in the direction of anti-tumor drugs, pharmaceutical formulations, medical preparations of non-active ingredients, etc., can solve the problems of uncontrollable release, low drug loading rate, and poor therapeutic effect, so as to improve the therapeutic effect , Improve the effect of drug loading

Inactive Publication Date: 2018-11-13
SOUTHWEST UNIVERSITY
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0004] In view of this, one of the objectives of the present invention is to provide a multi-stimuli-responsive synergistic anti-tumor polymer pro- Preparation method of medicine and its application in the field of drug treatment of cancer

Method used

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  • Preparation method of multi-stimulation-response cooperative anti-tumor polymer prodrug
  • Preparation method of multi-stimulation-response cooperative anti-tumor polymer prodrug
  • Preparation method of multi-stimulation-response cooperative anti-tumor polymer prodrug

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Embodiment 1

[0027] Example 1 Preparation of multi-stimuli-responsive star polymer prodrug CCDO

[0028] (1) Preparation of CPT precursor CPT-SS with reductive response: Under argon (Ar) atmosphere, ① 2-hydroxyethyl disulfide (BHD, 6.25g, 40.5mmol), tetrahydrofuran (THF, 50mL ) and triethylamine (TEA, 3.3mL, 24mmoL) were mixed and stirred, methacryloyl chloride (2.2mL, 22.73mmoL) was dissolved in 15 mL of anhydrous THF and added dropwise to the system, reacted overnight, and purified by column to obtain MABHD; ② Disperse the mixture of CPT (1.39g, 4mmoL) and 4-dimethylaminopyridine (DMAP, 1.56g, 11.3mmoL) into 70mL anhydrous DCM, and dissolve triphosgene (BTC, 500mg, 1.685mmoL) in 10 mL of anhydrous DCM, then added dropwise to the system, after 30min of reaction, then 10 mL of anhydrous THF containing MABHD (976mg, 2.375mmoL) was added dropwise to the system, stirred overnight, and purified to obtain the precursor CPT-SS;

[0029](2) Preparation of drug initiator β-CD-Br: Dissolve cyclod...

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Abstract

The invention discloses a preparation method of a multi-stimulation-response cooperative anti-tumor polymer prodrug. The preparation method comprises the following steps: based on beta-cyclodextrin, modifying a double-sulfur-bond camptothecin monomer CPT-SS, 2-(diisopropylamino)ethyl methacrylate DPA and polyethylene glycol methacrylate OEGMA on an initiator by utilizing atom transfer radical polymerization reaction (ATRP), so as to obtain an amphiphilic polymer prodrug beta-CD-P (CPT-co-DPA-co-OEGMA). The obtained amphiphilic polymer prodrug can be directly self-assembled in a water phase toform a single-molecule medicine micelle and also can be used for physical embedding an anti-cancer drug, i.e., adriamycin. Double sulfur bonds of the single-molecule prodrug are opened under the stimulation of a tumor microenvironment condition, amphiphilic performance is changed and the anti-tumor drug is synchronously released to kill tumor cells. Therefore, the method has the advantages that the loading amount of a hydrophobic drug is improved and the selectivity of the anti-tumor drug is also increased; the cooperative treatment effect is remarkable and the safety is high.

Description

technical field [0001] The invention belongs to the field of medicinal chemistry, and in particular relates to a preparation method of a multi-stimuli-responsive synergistic anti-tumor polymer prodrug and its application in the field of drug treatment of cancer. Background technique [0002] β-cyclodextrin (β-CD) is often used as an initiator to prepare star polymers by reversible addition-fragmentation chain transfer polymerization or atom transfer radical polymerization due to its good biocompatibility and biodegradability. . Camptothecin (CPT, chemical structural formula: C20H16N2O4, CAS number: 7689-03-4, relative molecular weight: 348.43) is a plant anticancer drug extracted from camptothecin distributed in south-central and southwest China. It has a good curative effect on gastrointestinal tract and head and neck cancer. Camptothecin is a cytotoxic quinoline alkaloid that inhibits DNA topoisomerase (TOPO I). Doxorubicin (Doxorubicin, DOX, chemical structural formula...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/69A61K31/4745A61K47/54A61K47/58A61K31/704A61P35/00
CPCA61K31/4745A61K31/704A61K47/542A61K47/58A61K47/6907A61P35/00A61K2300/00
Inventor 许志刚王亚君张天薛鹏康跃军
Owner SOUTHWEST UNIVERSITY
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