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Nano-enzyme modified polymer carrier and preparation method and antitumor nanoparticles thereof

A nano-enzyme and polymer technology, applied in the fields of nano-medicine and polymer chemistry, can solve the problems of unsatisfactory drug efficacy, difficulty in achieving specific drug release, high drug resistance, etc., and achieve the effect of multi-functionality

Active Publication Date: 2019-11-01
WENZHOU MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0003] However, although the existing targeted drug delivery system can be enriched at the tumor site, it is difficult to achieve the specific release of drugs using the tumor microenvironment
Moreover, tumor sites are more acidic and H-rich than normal tissues 2 o 2 The traditional delivery system aims to improve the shortcomings of the physical and chemical properties of the drug and complete the targeted drug delivery function at a specific site. Limited by the unique microenvironment, the drug effect is often not as expected, and it still has high drug resistance.

Method used

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  • Nano-enzyme modified polymer carrier and preparation method and antitumor nanoparticles thereof
  • Nano-enzyme modified polymer carrier and preparation method and antitumor nanoparticles thereof
  • Nano-enzyme modified polymer carrier and preparation method and antitumor nanoparticles thereof

Examples

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Embodiment 1

[0045] This embodiment provides a nanozyme-modified polymer carrier and a preparation method thereof, the steps are as follows:

[0046]Step 1. Dissolve 0.75g of 4-carboxyphenylboronic acid pinacol ester (PBA) in 50mL of dimethylsulfoxide (DMSO), then add 0.94g of dicyclohexylcarbodiimide (DCC) and 0.52g N-hydroxysuccinimide (NHS), stirred and activated for 2 hours to obtain an activated solution.

[0047] Step 2. Dissolve 0.06 g of polyethyleneimine (PEI) with a molecular weight of 800 Da in 50 ml of ultrapure water to obtain a PEI aqueous solution, move the activation solution to a constant pressure funnel, and slowly add it to the PEI aqueous solution while stirring at room temperature. Add the above-mentioned activating solution dropwise. After all the addition is completed, continue to stir for 24 hours to make the mixture into a homogeneous system with opalescence. Dialyze with a dialysis bag with a molecular weight cut-off of 8000Da and collect the sample after two days...

Embodiment 2

[0055] This embodiment provides a nanozyme-modified polymer carrier and a preparation method thereof, the steps are as follows:

[0056] Step 1. Dissolve 0.75g of 4-carboxyphenylboronic acid pinacol ester (PBA) in 55mL of dimethylsulfoxide (DMSO), then add 0.94g of dicyclohexylcarbodiimide (DCC) and 0.52g N-hydroxysuccinimide (NHS), stirred and activated for 2 hours to obtain an activated solution.

[0057] Step 2. Dissolve 0.11g of polyethyleneimine (PEI) with a molecular weight of 800Da in 55ml of ultrapure water to obtain a PEI aqueous solution, move the activation solution to a constant pressure funnel, and slowly add it to the PEI aqueous solution while stirring at room temperature. Add the above-mentioned activating solution dropwise. After all the addition is completed, continue to stir for 24 hours to make the mixture into a homogeneous system with opalescence. Dialyze with a dialysis bag with a molecular weight cut-off of 8000Da and collect the sample after two days t...

Embodiment 3

[0065] This embodiment provides a nanozyme-modified polymer carrier and a preparation method thereof, the steps are as follows:

[0066] Step 1. Dissolve 0.75g of 4-carboxyphenylboronic acid pinacol ester (PBA) in 60mL of dimethylsulfoxide (DMSO), then add 0.94g of dicyclohexylcarbodiimide (DCC) and 0.52g N-hydroxysuccinimide (NHS), stirred and activated for 2 hours to obtain an activated solution.

[0067] Step 2. Dissolve 0.33 g of polyethyleneimine (PEI) with a molecular weight of 800 Da in 60 ml of ultra-pure water to obtain a PEI aqueous solution, move the activation solution to a constant pressure funnel, and slowly add it to the PEI aqueous solution while stirring at room temperature. Add the above-mentioned activating solution dropwise. After all the addition is completed, continue to stir for 24 hours to make the mixture into a homogeneous system with opalescence. Dialyze with a dialysis bag with a molecular weight cut-off of 8000Da and collect the sample after two da...

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Abstract

The invention relates to a nano-enzyme modified polymer carrier and a preparation method and antitumor nanoparticles thereof. The preparation method of the nano-enzyme modified polymer carrier comprises the following steps of enabling 4-phenylboronic acid pinacol ester to dissolve in dimethyl sulfoxide, and adding an activator to obtain activated liquid; enabling polyethyleneimine to dissolve in water, adding the activated liquid, and performing stirring for the first time to obtain a first intermediate product; loading nano-enzymes on polysaccharide to obtain a second intermediate product; and adding the first intermediate product in the second intermediate product, and performing stirring for the second time to obtain the nano-enzyme modified polymer carrier. The polymer carrier preparedby the method can adsorb a functional molecule bearing negative charges, through self-assembly, stable nanoparticles are formed, under the condition that tumor tissues are high in H2O2 content and acid environment exists, specific release of medicine functional molecules in target positions can be realized, and besides, oxygen can be generated under the condition that the H2O2 content is higher and the acid environment exists. The hypoxia can be improved, and the drug tolerance can be reduced.

Description

technical field [0001] The invention relates to the fields of macromolecular chemistry and nanomedicine, in particular to a nanozyme-modified polymer carrier, a preparation method thereof, and anti-tumor nanoparticles. Background technique [0002] At the present stage, tumor diagnosis and treatment is an important direction of nanotechnology research, which is conducive to improving the drug response of the tumor microenvironment, involving the targeted release of tumor drugs and the immune response in the tumor microenvironment. The high targeting of tumor chemotherapy drugs can enrich the drugs in the tumor site, thereby reducing side effects, so the targeting of tumor chemotherapy drugs is a hot topic in current research. Moreover, due to the physiological characteristics of cell membranes, it is difficult for negatively charged drugs to enter cells and exert their killing effect on cells. Therefore, at present, the purpose of drug entry into cells is mostly achieved by...

Claims

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Application Information

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IPC IPC(8): A61K47/69A61K49/00A61K38/43A61K33/244A61P35/00B82Y5/00B82Y20/00B82Y30/00
CPCA61K47/6939A61K47/6933B82Y5/00B82Y20/00B82Y30/00A61P35/00A61K49/0034A61K49/0093A61K49/0056A61K49/0054A61K33/244A61K38/43A61K2300/00Y02A50/30
Inventor 师帅李星熠曾丽陈浩
Owner WENZHOU MEDICAL UNIV
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