Zwitter-ion-contained multiple acid-sensitive anti-tumor drug-loading micelle and preparation method and application thereof

A zwitterion, acid-sensitive technology, applied in the field of multiple acid-sensitive anti-tumor drug-loaded micelles and their preparation, can solve the problems of difficult to achieve drug treatment concentration, the inability of nanoparticles to respond quickly, etc., and achieve low toxic side effects and high sensitive response. Sexual and anti-tumor efficacy

Inactive Publication Date: 2016-09-28
SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there is only one sensitive bond in most nanomaterials. Nanoparticles cannot respond with high sensitivity and rapid response in the tumo

Method used

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  • Zwitter-ion-contained multiple acid-sensitive anti-tumor drug-loading micelle and preparation method and application thereof
  • Zwitter-ion-contained multiple acid-sensitive anti-tumor drug-loading micelle and preparation method and application thereof
  • Zwitter-ion-contained multiple acid-sensitive anti-tumor drug-loading micelle and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Example Embodiment

[0050] Example 1: Preparation of 2,2-bis(acryloyloxy-1-ethoxy)propane

[0051] First, hydroxyethyl acrylate and 2,2-dimethoxypropane are mixed in a molar ratio of 2:1, benzene and p-toluenesulfonic acid are added, and the benzene-methanol azeotrope is evaporated under the reaction conditions of 58℃. Out, get the initial product. The obtained initial product was purified by silica gel column chromatography, eluted with a mixed solvent of n-hexane and dichloroethane (1:1), and the eluent was removed by rotary evaporation to obtain a colorless oily liquid for purification. After the product ADA.

Example Embodiment

[0052] Example 2: Preparation of Carboxybetaine Methacrylate (CBMA)

[0053] Dissolve 0.11 mmol of 2-(dimethylamino) ethyl methacrylate in 50 mL of anhydrous acetone under vigorous stirring, and slowly add 0.14 mmol of β-propiolactone in 10 mL of anhydrous acetone under the protection of nitrogen Drop into the above solution. Under the protection of nitrogen, the reaction was carried out at 4°C for 5 hours to obtain a white powder. Then, the obtained white powder was washed with anhydrous acetone and anhydrous ether in sequence, and dried in a vacuum drying oven to obtain a white powdery product.

Example Embodiment

[0054] Example 3: Preparation of polycarboxybetaine methacrylate (pCBMA)

[0055] The ATRP method (atom transfer radical polymerization method) was used to prepare polycarboxybetaine methacrylate. The product synthesized in Example 2 was used as the reaction monomer, and ethyl 2-bromoisobutyrate was used as the initiator. , With 1,1,4,7,10,10-hexamethyltriethylenetetramine as the ligand, and the molar ratio of monomer:initiator:ligand=16.6:1:2 into a dry vial In, three vacuum-nitrogen cycles are performed to ensure the oxygen-free environment of the reaction system. Methanol:N,N-dimethylformamide (1:1) was injected into the reaction system with a syringe as the solvent, and cuprous bromide was added after three cycles of vacuum-nitrogen. The reaction system was sealed and reacted at 60°C for 24 h. The reaction system is connected to the air to terminate the reaction. The obtained initial reaction product is dialyzed in neutral water with a 500-1000 molecular weight cutoff dial...

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Abstract

The invention discloses a zwitter-ion-contained multiple acid-sensitive anti-tumor drug-loading micelle, and a preparation method and an application thereof, and belongs to the field of biological materials. The zwitter-ion-contained multiple acid-sensitive anti-tumor drug-loading micelle comprises a zwitter-ion hydrophilic shell and a lyophobic core containing two acid-sensitive bonds. The method includes the steps: separating methanol from hydroxyethyl acrylate and 2,2-dimethoxypropane and synthesizing 2,2-di(acryloyloxy-1-oxethyl) propane by an alcohol exchange method; connecting open-loop beta-propiolactone with 2-(dimethylamino) ethyl methacrylate to synthesize carboxybetaine methacrylate; obtaining a carboxybetaine methacrylate monomer polymer by an atom transfer free radical polymerization method; synthesizing triblock amphiphilic polymers by the atom transfer free radical polymerization method and a Michael addition one-pot method, and preparing the drug-loading nano-micelle by an ultrasonic drop method and a dialysis method. By aid of the drug-loading micelle, anti-tumor effects of chemotherapeutic drugs can be improved.

Description

technical field [0001] The invention belongs to the field of biological materials, in particular to a zwitterion-containing multiple acid-sensitive anti-tumor drug-loaded micelle, a preparation method and application thereof. technical background [0002] According to the statistics of the World Health Organization in 2013, tumors have become one of the major diseases threatening human health. Chemotherapy is currently one of the most commonly used and effective methods for clinical treatment of tumors. However, due to the lack of specific selection between tumor cells and normal cells, chemotherapy drugs also have strong toxicity, resulting in serious complications during the treatment process. toxic side effect. The emergence of nano-drug loading system has solved these problems well. Nanoparticles within a certain particle size range can use the enhanced penetration and retention effect (EPR effect) of tumor sites to enrich solid tumor sites through passive targeting; a...

Claims

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Application Information

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IPC IPC(8): C08G81/02C08G73/06A61K9/107A61K47/34A61K31/704A61P35/00
CPCA61K9/1075A61K31/704A61K47/34C08G73/0627C08G81/024
Inventor 顾忠伟马瑾易强英康珂
Owner SICHUAN UNIV
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