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Acid-responsive polycationic micelle nanoparticles and preparation method and application thereof

A micellar nano and polycation technology, which is applied in the direction of pharmaceutical formulations, medical preparations of non-active ingredients, powder delivery, etc., can solve problems such as limited curative effect

Inactive Publication Date: 2019-10-25
SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

At present, the commonly used means of clinical tumor treatment include surgery, chemotherapy, radiotherapy, etc., but the efficacy of the above means is limited, and it is urgent to develop new treatment strategies

Method used

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  • Acid-responsive polycationic micelle nanoparticles and preparation method and application thereof
  • Acid-responsive polycationic micelle nanoparticles and preparation method and application thereof
  • Acid-responsive polycationic micelle nanoparticles and preparation method and application thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0053] Embodiment 1: polyethylene glycol-polyglycidyl methacrylate diblock copolymer (mPEG 113 -b-PGMA 50 -Br) preparation

[0054] Take the polyethylene glycol macromolecular initiator (mPEG) of molecular weight 5000Da 113 -Br) 0.5 g was dissolved in 2.0 ml of N,N-dimethylacetamide (DMAC), 0.1 ml of isopropanol was added, stirred and mixed, and 1.78 ml of glycidyl methacrylate (GMA) was added, pentamethyl Diethylenetriamine 57 μl. After deoxygenation in vacuum, 7.8 mg of cuprous chloride catalyst was added and reacted at 40°C for 8 hours. After the reaction was completed, it was purified with an alumina column, concentrated by rotary evaporation, precipitated with ether, and dried with a vacuum pump to obtain 1.56 g of the product with a yield of 69%. Using deuterated chloroform as a solvent, the polymer structure was determined by H NMR spectroscopy as methoxy-terminated polyethylene glycol-polyglycidyl methacrylate (mPEG 113 -b-PGMA 50 -Br), see figure 1 .

Embodiment 2

[0055] Embodiment 2: polyethylene glycol-polyglycidyl methacrylate-polydiisopropylaminoethyl methacrylate triblock copolymer (mPEG 113 -b-PGMA 50 -b-PDPA 50 ) preparation

[0056] Get the methoxy-terminated polyethylene glycol-polyglycidylmethacrylate (mPEG) prepared in Example 2 113 -b-PGMA 50 -Br) 0.5 g was dissolved in 1.0 ml of DMAC, 0.1 ml of isopropanol was added, stirred and mixed, and then 1.31 ml of diisopropylaminoethyl methacrylate monomer and 12.6 microliters of pentamethyldiethylenetriamine were added. After deoxygenation, 6.7 mg of copper bromide catalyst was added, and reacted at 40° C. for 12 hours. After the reaction was completed, the copper salt was removed through an aluminum oxide column, concentrated by rotary evaporation at 40°C, precipitated with ether, and dried in vacuum to obtain 1.89 g of the product, with a yield of 92%. Using deuterated chloroform as a solvent, the structure of the polymer was confirmed by hydrogen nuclear magnetic resonance ...

Embodiment 3

[0057] Embodiment 3: Polyethylene glycol-ethylenediamine polyglycidyl methacrylate-polydiisopropylaminoethyl methacrylate polycation (mPEG 113 -b-PEDA 50 -b-PDPA 50 ) preparation

[0058] Get the mPEG prepared in embodiment 3 113 -b-PGMA 50 -b-PDPA 50 200mg, dissolved in 2ml DMAC. Dissolve 2.78 mL of ethylenediamine (DEA) in 3 mL of dry DMAC. The polymer solution was added dropwise to DEA, stirred and reacted at 80°C for 4 hours, then taken out, dialyzed for 24 hours with a dialysis bag with a molecular weight cut-off of 3500 Daltons (purchased from Shanghai Xinrui Biotechnology Co., Ltd.), and freeze-dried to obtain Product 113 mg, yield 62.5%, with deuterated dimethyl sulfoxide as solvent, the chemical structure of the polycation measured by proton nuclear magnetic resonance is mPEG 113 -b-PEDA 50 -b-PDPA 50 ,See figure 1 .

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Abstract

The invention belongs to the technical field of medical and chemical engineering, and particularly relates to acid-responsive polycation and a synthesis method thereof, and a preparation method of acid-responsive polycation micelle nanoparticles with acid sensitivity prepared from the acid-responsive polycation. The invention also relates to application of the multi-layered cationic micelle nanoparticles with double acid sensitivity to synchronous co-delivery of nucleic acid and molecular targeted drugs which are mainly used for gene therapy and immunotherapy of cancers. The acid-responsive polycation has the structure shown in formula 1 in specification.

Description

technical field [0001] The invention belongs to the technical field of medicine and chemical engineering, and specifically relates to an acid-responsive polycation and a synthesis method thereof, and a method for preparing acid-sensitive acid-responsive polycation micelle nanoparticles prepared from the acid-responsive polycation. The present invention also relates to the application of the multi-layered cationic micelle nanoparticle with double acid sensitivity for synchronous co-delivery of nucleic acid and molecular targeting drugs, mainly for gene and immunotherapy of cancer. Background technique [0002] Malignant tumor (referred to as tumor) is a serious disease that leads to death. At present, the commonly used means of clinical tumor treatment include surgery, chemotherapy, radiotherapy, etc., but the efficacy of the above means is limited, and the development of new treatment strategies is urgently needed. In recent years, immunotherapy has made great breakthroughs...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K9/107A61P35/00C08F8/32C08F293/00C08F220/34C08F220/32
CPCA61K9/1075A61K9/146A61K47/34A61P35/00C08F8/32C08F293/00C08F220/34
Inventor 于海军李亚平张汉武王当歌刘建萍王亭亭
Owner SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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