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Polymer carrier, preparation method of polymer carrier and anti-tumor nano particle

A nanoparticle and polymer technology, applied in the fields of nanomedicine and polymer chemistry, can solve the problems of low tumor targeting efficiency, lack of acid-base stability, and difficulty in achieving specific drug release, achieving multi-functionality. Chemical and chemically controllable effects

Active Publication Date: 2019-10-18
WENZHOU MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

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
In addition, the existing polyethyleneimine-phenylboronic acid nanostructures do not have acid-base stability, and can randomly and specifically adsorb with adjacent hydroxyl molecules, and the tumor targeting efficiency is not high.

Method used

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  • Polymer carrier, preparation method of polymer carrier and anti-tumor nano particle
  • Polymer carrier, preparation method of polymer carrier and anti-tumor nano particle
  • Polymer carrier, preparation method of polymer carrier and anti-tumor nano particle

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Embodiment 1

[0037] This embodiment provides a polymer carrier and its preparation method, see figure 1 ,Proceed as follows:

[0038] Step 1. Dissolve 0.25g of 4-carboxyphenylboronic acid pinacol ester (PBA) in 10mL of dimethylsulfoxide (DMSO), then add 0.312g of dicyclohexylcarbodiimide (DCC) and 0.174g N-hydroxysuccinimide (NHS), stirred and activated for 2 hours to obtain an activated solution.

[0039] Step 2. Dissolve 0.05g of polyethyleneimine (PEI) with a molecular weight of 800Da in 20mL 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 of 1000Da and collect the sample after two days to obtain the intermed...

Embodiment 2

[0042] This embodiment provides a method for preparing a polymer carrier, the steps are as follows:

[0043] Step 1. Dissolve 0.25g of 4-carboxyphenylboronic acid pinacol ester (PBA) in 10mL of dimethylsulfoxide (DMSO), then add 0.312g of dicyclohexylcarbodiimide (DCC) and 0.174g N-hydroxysuccinimide (NHS), stirred and activated for 2 hours to obtain an activated solution.

[0044] Step 2. Dissolve 0.22 g of polyethyleneimine (PEI) with a molecular weight of 2000 Da in 20 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 activating solution dropwise, and continue stirring for 48 hours after the addition is complete, so that the mixture becomes a homogeneous system with opalescence, dialyze with a dialysis bag with a molecular weight of 3000Da for two days, and collect the sample to obtain the intermediate product PEI-...

Embodiment 3

[0047] This embodiment provides a method for preparing a polymer carrier, the steps are as follows:

[0048] Step 1. Dissolve 0.25g of 4-carboxyphenylboronic acid pinacol ester (PBA) in 10mL of dimethylsulfoxide (DMSO), then add 0.312g of dicyclohexylcarbodiimide (DCC) and 0.174g N-hydroxysuccinimide (NHS), stirred and activated for 2 hours to obtain an activated solution.

[0049] Step 2. Dissolve 0.01 g of polyethyleneimine (PEI) with a molecular weight of 25,000 Da in 20 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 activating solution dropwise, and continue to stir for 24 hours after the addition is complete, so that the mixture becomes a homogeneous system with opalescence, dialyze with a dialysis bag with a molecular weight of 14000Da for two days, and collect the sample to obtain the intermediate product PE...

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Abstract

The invention relates to a polymer carrier, a preparation method of the polymer carrier and an anti-tumor nano particle. The preparation method of the polymer carrier comprises the following steps that 4-carboxyl phenylboronic acid pinacol ester is dissolved in dimethyl sulfoxide, and an activating agent is added to obtain activate liquid; polyethyleneimine is dissolved in water, then the activateliquid is added, and stirring for the first time is carried out to obtain an intermediate product; and hyaluronic acid is dissolved in the water, then the intermediate product is added, and stirringfor the second time is carried out to obtain the polymer carrier. The polymer carrier obtained by the method can adsorb medicine functional molecular bearing a negative charge to form the stable nanoparticle in a self-assembly mode, tumor height targeting ability is achieved, and specificity release of the medicine functional molecular at target parts is realized under the condition of higher H2O2 content of tumor tissue and an acid environment.

Description

technical field [0001] The invention relates to the fields of polymer chemistry and nanomedicine, in particular to a polymer carrier, a preparation method thereof, and anti-tumor nanoparticles. Background technique [0002] At this stage, tumor diagnosis and treatment is an important direction of nanotechnology research. 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 designing and constructing drug delivery carriers. [0003] However, although the existing targeted drug delivery system can be enriched at the tumor site, it is difficult to realize the specific release of drugs...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08G81/00C08L87/00A61K47/36A61K47/34A61K9/51A61K49/00
CPCA61K9/5146A61K9/5161A61K49/0034A61K49/0054A61K49/0093C08G81/00C08L87/005
Inventor 师帅曾丽李星熠陈浩
Owner WENZHOU MEDICAL UNIV
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