Nanometer medicine for improving tumor microenvironment based on hydralazine as well as preparation and application of nanometer medicine

A tumor microenvironment and nano-drug technology, applied in the field of nano-drugs and their preparation, can solve the problems of low therapeutic effect and limited pharmacokinetic properties, and achieve the effects of low toxicity, enhanced tumor selectivity, and enhanced therapeutic effect

Active Publication Date: 2022-03-01
ZHEJIANG UNIV HANGZHOU GLOBAL SCI & TECH INNOVATION CENT
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, bortezomib is less effective against many solid tumors due to significant dose-dependent toxicities such as peripheral neuropathy, thrombocytopenia, and gastrointestinal disorders
Also, bortezomib has limited pharmacokinetic properties due to its nonspecific binding to proteins and rapid clearance from the blood

Method used

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  • Nanometer medicine for improving tumor microenvironment based on hydralazine as well as preparation and application of nanometer medicine
  • Nanometer medicine for improving tumor microenvironment based on hydralazine as well as preparation and application of nanometer medicine
  • Nanometer medicine for improving tumor microenvironment based on hydralazine as well as preparation and application of nanometer medicine

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Experimental program
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Embodiment 1

[0048] 1. Preparation of nanomedicines

[0049] (1) p-aminoacetophenone (4.0 g, 29.6 mmol), methacryloyl chloride (3.6 g, 34.4 mmol) and triethylamine (4.0 g, 39.6 mmol) were dissolved in dichloromethane (DCM, 100 mL) and cooled with an ice bath. The mixture was stirred for 12 hours, then washed successively with saturated sodium bicarbonate solution, hydrochloric acid, distilled water and saturated sodium chloride solution, the solvent was removed by rotary evaporation, the N-(4-acetylphenyl)methacrylamide was isolated and washed with silica gel Purification by chromatography (n-hexane:ethyl acetate=4:1). The final polymerizable monomer after vacuum drying was 2.8 g (yield 46.7%). The reaction process is:

[0050]

[0051] (2) The polymer PAA is obtained by RAFT polymerization. Take the polymerizable monomer N-(4-acetylphenyl) methacrylamide (0.30g, 1.5mmol) obtained in the previous step, the macromolecular chain transfer agent PETTC-PEG 5k (0.27 g, 0.05 mmol) and AIB...

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Abstract

The invention discloses a nano-drug for improving a tumor microenvironment based on hydralazine as well as preparation and application of the nano-drug, and belongs to the technical field of medicines. The nano-drug is a micelle type nano-particle formed by self-assembling an amphiphilic polymer and a hydrophobic chemotherapeutic drug containing a boric acid group in water; a hydrophilic segment of the amphiphilic polymer is polyethylene glycol, and a hydrophobic segment of the amphiphilic polymer is a polymer formed by connecting a pH response type hydralazine bond with hydralazine. The nano-drug can efficiently release small-molecule hydralazine in an acidic tumor environment, and hydralazine improves the efficiency of conveying an entrapped chemotherapeutic drug to tumor tissues by expanding tumor blood vessels. In addition, the nano-drug can efficiently load chemotherapeutic drugs, and is intensively released in tumor acidic tissues, so that the treatment effect of the chemotherapeutic drugs is enhanced, the toxicity to normal tissues is low, and the tumor selectivity of the nano-drug is remarkably enhanced.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a nanomedicine based on hydralazine for improving the tumor microenvironment and enhancing the effect of chemotherapy, and a preparation method and application thereof. Background technique [0002] Nanoparticles have become an alternative to non-targeted chemotherapeutics due to their enhanced permeability and retention effect (EPR effect) and effective reduction of the toxic and side effects of chemotherapeutic drugs. However, the clinical translation of these nanomedicines is greatly limited, mainly due to the complex tumor microenvironment. As a major component of the tumor microenvironment, tortuous and complex tumor blood vessels are a major obstacle to nanoparticle delivery. Therefore, in order to improve the therapeutic effect of nanoparticles and promote their clinical translation, it is urgent to develop new strategies to improve the tumor microenvironment to enhance ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/69A61K47/60A61K31/502A61K31/69A61K38/05A61P35/00B82Y5/00B82Y40/00
CPCA61K47/6935A61K47/60A61K31/502A61K31/69A61K38/05A61P35/00B82Y5/00B82Y40/00A61K2300/00Y02A50/30
Inventor 唐建斌王睿徐晓丹
Owner ZHEJIANG UNIV HANGZHOU GLOBAL SCI & TECH INNOVATION CENT
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