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PtBA-b-PEG-b-PtBA block copolymer, and preparation method and application thereof

An a-b-b-b-a, block copolymer technology, applied in the direction of pharmaceutical formulations, drug combinations, medical preparations with non-active ingredients, etc., can solve the problems of easy shedding of target molecules and low polymer targeting efficiency, etc., and achieve excellent hydrophilicity. Effect

Inactive Publication Date: 2012-10-17
THE NAT CENT FOR NANOSCI & TECH NCNST OF CHINA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, the research on targeted drug release of functionalized polymers mainly uses the method of physical adsorption embedding to modify the targeting molecules on the polymers, but through simple physical modification, the targeting efficiency of the polymers is not high, and the target molecules may be easily Problems such as shedding

Method used

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  • PtBA-b-PEG-b-PtBA block copolymer, and preparation method and application thereof
  • PtBA-b-PEG-b-PtBA block copolymer, and preparation method and application thereof
  • PtBA-b-PEG-b-PtBA block copolymer, and preparation method and application thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0037] (1) Preparation of bromopolyethylene glycol macroinitiator: in one or two round-bottomed flasks, under the condition of nitrogen gas, 2 g of polyethylene glycol with a molecular weight of 6000 was dissolved in 20 mL of anhydrous toluene (sodium / diphenyl Ketone system refluxed to remove water), a small amount of water in polyethylene glycol 6000 was removed by azeotropic distillation with toluene. Cool the reaction system to 0°C, add 1.4mL redistilled triethylamine into the flask under stirring, keep the system at 0°C, add 0.124mL 2-bromoisobutyryl bromide dropwise to the flask, and cover the flask with tinfoil Avoid light. After stirring at room temperature for 24 h, the reaction was stopped. The white solid was filtered off, the solvent toluene was removed by rotary evaporation, the crude product was added to water and extracted 3 times with dichloromethane, precipitated with excess anhydrous ether, and dried in vacuo to obtain polyethylene glycol bifunctional bromina...

Embodiment 2

[0044] (1) In the preparation of bromopolyethylene glycol macroinitiator, select dichloromethane as solvent, and the reaction time is 48h, and other is with embodiment 1.

[0045] (2) The generation of block copolymer: device and operation are the same as embodiment 1, with polyethylene glycol macroinitiator 0.2g i.e. 0.03mmol, and monomer tert-butyl acrylate 0.79mL i.e. 5.4mmol, ligand PMDETA13 μ L i.e. Add 0.06mmol into the Schlenk tube, under the protection of nitrogen, freeze in liquid nitrogen-vacuumize-dissolve three times to remove the oxygen in the system; then add the catalyst cuprous bromide 9mg (0.06mmol) Stir in an oil bath at ℃ for 8 hours. After the reaction, the product is diluted with toluene and passed through a neutral alumina column to remove copper salts. Unpolymerized small molecule monomers and solvents are removed under reduced pressure, and vacuum-dried to obtain poly(tert-butylacrylate-polyacrylate) Ethylene glycol-tert-butyl polyacrylate triblock copo...

Embodiment 3

[0047] (1) In the preparation of bromopolyethylene glycol macroinitiator, reacted 36 hours, other are with embodiment 1.

[0048] (2) Generation of block copolymer: device and operation are the same as embodiment 1, with polyethylene glycol macroinitiator 0.2g 0.03mmol, and monomer tert-butyl acrylate 1.23mL i.e. 8.4mmol, ligand PMDETA13 μ L i.e. 0.06 Add mmol to the Schlenk tube, under the protection of nitrogen, freeze in liquid nitrogen-vacuumize-dissolve three times to remove the oxygen in the system; then add the catalyst cuprous bromide 9mg (0.06mmol), and place the reaction system at 90°C Stir in an oil bath for 12 hours. After the reaction, the product is diluted with toluene and passed through a neutral alumina column to remove copper salts. Unpolymerized small molecule monomers and solvents are removed under reduced pressure, and vacuum-dried to obtain poly(tert-butylacrylate-polyethylene) Diol-polyacrylate tert-butyl triblock copolymer, its structural formula is for...

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Abstract

The invention provides a poly(tert-butyl acrylate)-b-polyethylene glycol-b-poly(tert-butyl acrylate) block copolymer. The block copolymer comprises a hydrophilic intermediate block and a hydrophobic end blocks, and has a formula (I) of A-b-B-b-A (I). A represents poly(tert-butyl acrylate) chain segment as the hydrophobic end blocks; B represents polyethylene glycol as the hydrophilic intermediate block; and b represents a group connecting A to B. The method is as below: acyl bromide polyethylene glycol acyl is used as an initiator to initiate an ATRP polymerization of tert-butyl acrylate. After targeting molecular modification, an end of a backbone chain of the block copolymer can be used as a targeting antitumor drug carrier.

Description

technical field [0001] The present invention relates to a kind of block copolymer, relate in particular to a kind of polytert-butyl acrylate-b-polyethylene glycol-b-polyacrylate tert-butyl ester (PtBA-b-PEG-b-PtBA) block copolymer and The preparation method and application thereof belong to the preparation technology of amphoteric tri-block copolymers. Background technique [0002] Block copolymers are homopolymeric segments composed of different structural units, which are covalently bonded to each other to form a main chain. Each chain segment contains only one kind of structural unit, and there can be two or more different homopolymeric chain segments. Due to the different physical and chemical properties of different segments, block copolymers often exhibit special and excellent properties that many homopolymers do not possess. [0003] Block copolymers with controllable molecular weight, narrow molecular weight distribution, and designable molecular structure and comp...

Claims

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Application Information

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IPC IPC(8): C08F293/00C08F220/18C08G65/48A61K47/32A61P35/00
Inventor 宫建茹刘倩
Owner THE NAT CENT FOR NANOSCI & TECH NCNST OF CHINA
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