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Doxorubicin prodrug for combined use of tumor penetration enhanced photo-thermal and chemotherapy and preparation method of doxorubicin prodrug

A technology for enhancing penetration and doxorubicin is applied in the field of doxorubicin prodrug and its preparation, which can solve the problems of reducing the efficacy of chemotherapeutic drugs, and achieve the effects of avoiding early release and improving drug utilization rate.

Active Publication Date: 2022-03-22
HUAIYIN INSTITUTE OF TECHNOLOGY
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Drugs coated by physical coating are often unable to avoid early entry into the blood due to diffusion during delivery, resulting in toxic side effects
The formation of drug prodrugs by chemical bond connection is a good way to solve the above problems. However, under normal circumstances, what is released after the controlled release of general chemotherapeutic drug prodrugs may not be the chemotherapeutic drug itself, and there will be certain functional group modifications. The efficacy of chemotherapy drugs will be greatly reduced

Method used

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  • Doxorubicin prodrug for combined use of tumor penetration enhanced photo-thermal and chemotherapy and preparation method of doxorubicin prodrug
  • Doxorubicin prodrug for combined use of tumor penetration enhanced photo-thermal and chemotherapy and preparation method of doxorubicin prodrug
  • Doxorubicin prodrug for combined use of tumor penetration enhanced photo-thermal and chemotherapy and preparation method of doxorubicin prodrug

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Experimental program
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Embodiment 1

[0037]1) Preparation of DOX-photothermal conversion nanoparticles: 0.1 mmol DOX hydrochloride and 0.1 mmol NPC-PEG-SH (molecular weight 1 KDa) were dissolved in 3 mL DMF, and the reaction mixture was stirred at room temperature under nitrogen atmosphere for 18 hours. After purification, DOX-NH-COO-PEG-SH was produced. Then connect 20 mg of near-infrared photothermal conversion material copper sulfide to the thiol end to obtain DOX-photothermal conversion nanoparticles;

[0038] 2) Preparation of pHPP nanocarrier: Dissolve 0.1mol PCL-COOH (molecular weight 11.4KDa) in N,N-dimethylformamide (DMF), then add the same molar amount of EDC and NHS, react at room temperature for 2-3 hours to activate the carboxyl group on PCL-COOH, then add 0.3mmol of N 2 h 4 ·H 2 O was reacted overnight. It was then dialyzed against deionized water and lyophilized to obtain pHPNN. PEG-ALD (molecular weight 5KDa) and pHPNN were mixed and dissolved in ethanol in equimolar amounts, and heated to re...

Embodiment 2

[0041] 1) Preparation of DOX-photothermal conversion nanoparticles: 0.1 mmol DOX hydrochloride and 0.09 mmol NPC-PEG-SH (molecular weight 5K Da) were dissolved in 3 mL DMF, and the reaction mixture was stirred at room temperature under nitrogen atmosphere for 18 hours. After purification, DOX-NH-COO-PEG-SH was produced. Then connect 30 mg of near-infrared photothermal conversion material gold nanorods with the thiol end to obtain DOX-photothermal conversion nanoparticles;

[0042] 2) Preparation of pHPP nanocarrier: Dissolve 0.1mol PCL-COOH (molecular weight 10K Da) in N, N-dimethylformamide (DMF), then add the same molar amount of EDC and NHS, and react at room temperature for 2- 3 hours to activate the carboxyl group on PCL-COOH, then add 0.25mmol N 2 h 4 ·H 2 O was reacted overnight. It was then dialyzed against deionized water and lyophilized to obtain pHPNN. PEG-ALD (molecular weight 2K Da) and pHPNN were mixed and dissolved in ethanol in equimolar amounts, and heate...

Embodiment 3

[0045] 1) Preparation of DOX-photothermal conversion nanoparticles: 0.1 mmol DOX hydrochloride and 0.11 mmol NPC-PEG-SH (molecular weight 8 KDa) were dissolved in 3 mL DMF, and the reaction mixture was stirred at room temperature under nitrogen atmosphere for 18 hours. After purification, DOX-NH-COO-PEG-SH was prepared, and 40 mg of near-infrared photothermal conversion material copper sulfide was connected to the thiol end to obtain DOX-photothermal conversion nanoparticles;

[0046] 2) Preparation of pHPP nanocarrier: Dissolve 0.1mmol PCL-COOH (molecular weight 5K Da) in DMF, then add the same molar amount of EDC and NHS, and react at room temperature for 2 to 3 hours to activate the carboxyl group on PCL-COOH , then add 0.4mmol N 2 h 4 ·H 2 O was reacted overnight. It was then dialyzed against deionized water and lyophilized to obtain pHPNN. PEG-ALD (molecular weight 5K Da) and pHPNN were mixed and dissolved in ethanol at a molar ratio of 1:1.1, and heated to reflux for...

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Abstract

The invention discloses an adriamycin prodrug for combined use of tumor penetration enhanced photothermal and chemotherapy and a preparation method of the adriamycin prodrug. The preparation method comprises the following steps: after DOX and NPC-PEG-SH react, connecting a sulfydryl end with a photothermal conversion material to synthesize DOX-photothermal conversion nanoparticles; further, a hydrazone bond is introduced into PEG and PCL to prepare pHPP; finally, the DOX-photothermal conversion nanoparticles are coated with the pHPP, and the DOX prodrug is prepared. The nano-drug prepared by the invention has the characteristic of combined use of photothermal and chemotherapy with enhanced in-tumor permeation, and can more effectively resist tumor cells. The nano-drug has an intelligent size regulation strategy, has a large size in blood to enhance long circulation, is disintegrated into small-size DOX-photothermal conversion nano-particles in a tumor to enhance permeation, and can generate heat under near-infrared illumination to release DOX after penetrating into the deep part of the tumor, so as to achieve the purpose of enhancing the penetration of the DOX-photothermal conversion nano-particles. Therefore, the aim of combining photo-thermal and chemotherapy is fulfilled.

Description

technical field [0001] The invention belongs to the technical field of biomedical polymer materials, and in particular relates to a doxorubicin prodrug used in combination with tumor penetration enhancing photothermal and chemotherapy and a preparation method thereof. Background technique [0002] Nanomedicine was once considered to be an effective way to solve tumor chemotherapy, because of its advantages such as endowing chemotherapy drugs with targeting, improving drug solubility, prolonging the half-life of drugs in the body, reducing the immunogenicity of drugs, and promoting transcellular transport of drugs, etc. Advantage. The use of nanocarriers has improved the therapeutic effect of chemotherapy to a certain extent, but in recent years there have been major doubts, and many nanomedicines (for example: doxorubicin liposome ) can be effectively enriched in the tumor, but the improvement of the clinical treatment effect is not obvious. [0003] In recent years, some...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K41/00A61K9/51A61K47/60A61P35/00A61K31/704
CPCA61K41/0042A61K41/0052A61K31/704A61K47/60A61K9/5153A61P35/00A61K2300/00
Inventor 沈灿姜东升柳森钱程刘楠楠邓帅靖刘希龙徐航王智豪汤雪聪张怡然叶玮
Owner HUAIYIN INSTITUTE OF TECHNOLOGY
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