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Taxane drug and doxorubicin prodrug self-assembled nanoparticles and application thereof

A technology for self-assembling nanoparticles and taxanes, which is used in the preparation of taxane drugs-adriamycin prodrug self-assembled nanoparticles, application in drug delivery systems, taxane drugs-doxorubicin In the field of self-assembled nanoparticles of prodrugs, it can solve the problems of suboptimal efficacy, inconsistent release rate, and sudden release, and reduce the effect of intravenous injection.

Active Publication Date: 2020-12-18
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, they often have low drug loading, often have burst release phenomenon or are difficult to release from polymers, and the release speed of the two drugs will not be consistent, resulting in less than optimal curative effect. Therefore, the invention is safe, simple and efficient New approach to co-deliver taxanes and doxorubicin is needed

Method used

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  • Taxane drug and doxorubicin prodrug self-assembled nanoparticles and application thereof
  • Taxane drug and doxorubicin prodrug self-assembled nanoparticles and application thereof
  • Taxane drug and doxorubicin prodrug self-assembled nanoparticles and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0068] Embodiment 1: the synthesis of paclitaxel-doxorubicin prodrug PTX-C-DOX

[0069] A certain amount of paclitaxel and glutaric anhydride were dissolved in a small amount of dichloromethane, and under the catalysis of 4-dimethylaminopyridine (DMAP), the reaction was stirred at room temperature under nitrogen protection for 24 hours. After the reaction was completed, the reaction solution was washed three times with saturated brine. Separation of CH 2 Cl 2 layer and dried over anhydrous sodium sulfate, filtered, concentrated and evaporated to dryness with a rotary evaporator, separated and purified to obtain intermediate 1 as a white solid. Appropriate amount of intermediate 1 and doxorubicin were mixed in dichloromethane, added HBTU and DIPEA and stirred together, and stirred under nitrogen for 1 day. After the reaction, the dichloromethane layer was washed three times with saturated brine, dried over anhydrous sodium sulfate, filtered, evaporated to dryness, and separat...

Embodiment 2

[0071] Example 2: Synthesis of Paclitaxel-Adriamycin prodrug PTX-S-DOX linked by redox double sensitive thioether bond

[0072] Dissolve an appropriate amount of paclitaxel and thioglycolic anhydride in a small amount of dichloromethane, under the catalysis of 4-dimethylaminopyridine (DMAP), stir and react at room temperature under nitrogen protection for 24 hours, after the reaction is completed, wash the reaction solution with saturated brine three times , the CH2Cl2 layer was separated and dried with anhydrous sodium sulfate, filtered, concentrated and evaporated to dryness with a rotary evaporator, and separated and purified to obtain intermediate 2 as a white solid. Appropriate amount of intermediate 2 and doxorubicin were mixed in dichloromethane, added HBTU and DIPEA and stirred together, and stirred under nitrogen for 1 day. After the reaction, the dichloromethane layer was washed three times with saturated brine, dried over anhydrous sodium sulfate, filtered, evaporat...

Embodiment 3

[0074] Embodiment 3: the synthesis of docetaxel-doxorubicin prodrug DTX-C-DOX

[0075]Dissolve a certain amount of docetaxel and glutaric anhydride in a small amount of dichloromethane, and under the catalysis of 4-dimethylaminopyridine (DMAP), stir and react at room temperature under nitrogen protection for 24 hours. After the reaction, the reaction solution is washed with saturated brine After washing three times, the CH2Cl2 layer was separated and dried with anhydrous sodium sulfate, filtered, concentrated and evaporated to dryness with a rotary evaporator, separated and purified to obtain intermediate 3 as a white solid. An appropriate amount of intermediate 3 and doxorubicin were mixed in dichloromethane, added with HBTU and DIPEA and stirred together, and stirred under nitrogen for 1 day. After the reaction, the dichloromethane layer was washed three times with saturated brine, dried over anhydrous sodium sulfate, filtered, evaporated to dryness, and separated and purifi...

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Abstract

The invention belongs to the field of new auxiliary materials and new dosage forms of pharmaceutical preparations, relates to taxane drug and doxorubicin prodrug self-assembled nanoparticles and application thereof, and in particular relates to synthesis of a redox sensitive taxane drug and doxorubicin prodrug with tumour tissue specific response, preparation of the taxane drug and doxorubicin prodrug self-assembled nanoparticles and application of the taxane drug and doxorubicin prodrug self-assembled nanoparticles in a drug delivery system. The taxane drug and doxorubicin prodrug in the invention comprises a taxane drug and doxorubicin prodrug connected with a carbon chain and a taxane drug and doxorubicin prodrug connected with a redox sensitive thioether bond; and the structural general formula of the taxane drug and doxorubicin prodrug is shown in the specification, wherein R<1>, R<2>, X, Y, Z, n<1> and n<2> are described in the claims and the specification.

Description

technical field [0001] The invention belongs to the field of new auxiliary materials and new dosage forms of pharmaceutical preparations, and relates to taxane drug-doxorubicin prodrug self-assembled nanoparticles and applications thereof. It specifically relates to the synthesis of redox-sensitive taxane drug-doxorubicin prodrug with tumor tissue specific response and the preparation of taxane drug-doxorubicin prodrug self-assembled nanoparticles, and its application in drug delivery system in the application. Background technique [0002] At present, chemotherapy is still the mainstay of clinical tumor treatment. However, clinical studies have shown that a single chemotherapy drug is prone to multidrug resistance and has poor efficacy on solid tumors. In addition, due to the insignificant effect of a single chemotherapy drug, it leads to increased drug dosage or medication time. Prolongation will increase the toxic and side effects of the drug. Therefore, combination the...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/55A61K31/704A61K47/69A61K47/60A61P35/00A61K31/337
CPCA61K47/55A61K31/337A61K31/704A61P35/00A61K47/6935A61K2300/00
Inventor 王永军王颖丽刘洪卓何仲贵
Owner SHENYANG PHARMA UNIVERSITY
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