A kind of tumor actively targeting star-shaped amphiphilic polymer micelle nanomedicine and preparation method thereof

A technology of amphiphilic polymers and star polymers, which can be used in antineoplastic drugs, drug combinations, pharmaceutical formulations, etc., and can solve problems such as no obvious improvement in curative effect, no curative effect, and reduced curative effect

Active Publication Date: 2020-07-07
LINYI UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0003] However, for many polymer micellar nanomedicines, although the toxic and side effects can be reduced to a certain extent, the curative effect is not significantly improved compared with the original drug.
The reason is that nanomedicine needs to face the interference of various factors in the long-distance transportation of the human circulatory system, such as blood washing and dilution, organ clearance and various enzymatic hydrolysis, etc. Decomposition occurs prematurely, making it difficult for the drug to be transported into the lesion cells, resulting in reduced or even no curative effect

Method used

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  • A kind of tumor actively targeting star-shaped amphiphilic polymer micelle nanomedicine and preparation method thereof
  • A kind of tumor actively targeting star-shaped amphiphilic polymer micelle nanomedicine and preparation method thereof
  • A kind of tumor actively targeting star-shaped amphiphilic polymer micelle nanomedicine and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] A preparation method of star-shaped amphiphilic polymer micelle nanomedicine with active tumor targeting:

[0037] (1) Preparation of ATRP-initiated monomers: add 1.35 g of trimethylolpropane, 3 g of dehydrated triethylamine and 100 mL of dichloromethane into a round-bottomed flask, cool to 0°C, and dropwise add 14 g of 2-bromoiso Butyryl bromide, the dropwise addition time was controlled to 2h, after the dropwise addition, the reaction was continued at 0°C for 2h, and then the temperature was slowly raised to 30°C for 48h. After the reaction, the product was washed three times with saturated sodium bicarbonate solution, saturated brine and deionized water respectively, and the organic phase was dried with anhydrous magnesium sulfate, and the ATRP initiating monomer (S-Br) was obtained by rotary evaporation and drying. 3 ).

[0038] (2) Star polymer [S(PGA) 3 ]: 0.058 g ATRP initiating monomer (S-Br 3 ) and 0.43 g of glycidyl methacrylate (GMA) were dissolved in 20 m...

Embodiment 2

[0042] A preparation method of star-shaped amphiphilic polymer micelle nanomedicine with active tumor targeting:

[0043] (1) Preparation of ATRP-initiated monomers: add 1.35 g of trimethylolpropane, 3 g of dehydrated triethylamine and 100 mL of dichloromethane into a round-bottomed flask, cool to 0°C, and dropwise add 14 g of 2-bromoiso Butyryl bromide, the dropwise addition time was controlled to 2h, after the dropwise addition, the reaction was continued at 0°C for 2h, and then the temperature was slowly raised to 30°C for 48h. After the reaction, the product was washed three times with saturated sodium bicarbonate solution, saturated brine and deionized water respectively, and the organic phase was dried with anhydrous magnesium sulfate, and the ATRP initiating monomer (S-Br) was obtained by rotary evaporation and drying. 3 ).

[0044] (2) Star polymer [S(PGA) 3 ]: 0.058 g ATRP initiating monomer (S-Br 3 ) and 0.85 g of glycidyl methacrylate (GMA) were dissolved in 20 m...

Embodiment 3

[0048] A preparation method of star-shaped amphiphilic polymer micelle nanomedicine with active tumor targeting:

[0049] (1) ATRP (S-Br 4 ) to initiate monomer preparation: 1.36g of pentaerythritol, 4g of dehydrated triethylamine and 100mL of dichloromethane were added to a round-bottomed flask, cooled to 0°C, and 18.4g of 2-bromoisobutyryl bromide was added dropwise. The addition time was controlled to 2h, after the dropwise addition, the reaction was continued at 0°C for 2h, and then the temperature was slowly raised to 30°C for 48h. After the reaction, the product was washed three times with saturated sodium bicarbonate solution, saturated brine and deionized water respectively, and the organic phase was dried with anhydrous magnesium sulfate, and the ATRP initiating monomer was obtained by rotary evaporation and drying.

[0050] (2) Star polymer [S(PGA) 4 ]: 0.073 g ATRP initiating monomer (S-Br 4 ) and 0.56 g of glycidyl methacrylate (GMA) were dissolved in 20 mL of a...

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Abstract

The invention discloses a star-shaped amphiphilic polymer and a preparation method thereof and a nano drug with a constructed micelle of the star-shaped amphiphilic polymer as a carrier. The star-shaped amphiphilic polymer is prepared by adopting polyhydric alcohol as an inner core, initiating the polymerization of glycidyl methacrylate (GMA) through activation, and then utilizing an active epoxyfunctional group to react with an amine-terminated hydrophobic chain segment (A-NH2) and targeting group (B) modified polyethylene glycol (B-PEG-NH2) separately. Polylactic acid (PLA-NH2) or polycaprolactone (PCL-NH2) is preferably selected as the hydrophobic chain segment, and anisamide (Anis) or phenylboronic acid (PBA) is preferably selected as the targeting group. According to the star-shapedamphiphilic polymer prepared by the method, the raw materials are cheap and easy to obtain, the biocompatibility is great, and the preparation process is relatively simple and easy. At the same time,the nano drug with the constructed micelle of the star-shaped amphiphilic polymer as the carrier can have long circulation in the blood and an active targeting function, and therefore the nano drug has a good anti-tumor effect.

Description

technical field [0001] The invention relates to the technical field of the preparation of functional polymer materials and anti-tumor drugs, in particular to a tumor-targeting star-shaped amphiphilic polymer micelle nano-drug and a preparation method thereof. Background technique [0002] In recent years, with the rapid development of nano-biomedical technology, nano-drugs can just solve the shortcomings of tumor chemotherapy. Therefore, nano-drugs have great potential in the clinical treatment of tumors. Nanomedicine is generally composed of a carrier and an antitumor drug. The drug plays a therapeutic role, and the carrier plays a role in embedding the drug and delivering it. Among them, nanomedicines based on polymer micelles have become the current research hotspot due to their good biocompatibility, degradability, and easy structure modification. Up to now, a variety of polymer micelle nanomedicines have entered the clinical trial stage, such as paclitaxel-loaded polye...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/107A61K31/337A61K31/4745A61K31/704A61K47/34A61P35/00C08G81/02
CPCA61K9/1075A61K31/337A61K31/4745A61K31/704A61K47/34C08G81/025
Inventor 李因文李依娉汤玉琪刘大泰薛光宇于梦贤高庆超
Owner LINYI UNIVERSITY
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