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Triblock copolymer polyethyleneimine (PEI)-polyethylene glycol (PEG)-PEI

A PEI-PEG-PEI, triblock technology, used in genetic material components, medical preparations with non-active ingredients, gene therapy, etc., can solve the problems of toxicity, transfection efficiency lower than viral vectors, etc., to improve the response Activity, improved gene transfection efficiency, and low cytotoxicity

Inactive Publication Date: 2013-07-31
方剑群
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0007] Aiming at the problem that cationic polymers used as gene drug carriers in the prior art have charge-related toxicity to cells, and the transfection efficiency is lower than that of viral vectors, the present invention provides a triblock copolymer PEI-PEG-PEI, which The technical solution started from increasing the molecular weight of polyethyleneimine while reducing its biological toxicity, and successfully synthesized a triblock of PEI-PEG-PEI (polyethyleneimine-polyethylene glycol-polyethyleneimine) with different chain lengths. Polymer, the polymer has the characteristics of high transfection rate and low cytotoxicity, and has broad application prospects

Method used

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  • Triblock copolymer polyethyleneimine (PEI)-polyethylene glycol (PEG)-PEI
  • Triblock copolymer polyethyleneimine (PEI)-polyethylene glycol (PEG)-PEI
  • Triblock copolymer polyethyleneimine (PEI)-polyethylene glycol (PEG)-PEI

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Embodiment 1

[0024] combine figure 1 , a kind of triblock copolymer PEI-PEG-PEI of present embodiment 1, its structural formula is as follows:

[0025]

[0026] Such as figure 1 The synthetic process of above-mentioned triblock copolymer PEI-PEG-PEI synthetic method, its step is:

[0027] (1) the PEG k 、Et 3 N and Me 3 Take 5mol, 20mol, and 1mol of N.HCl according to the molar ratio of 5:20:1, and dissolve them in 40ml of CH 2 Cl 2 Among them, the molecular weight k=1000;

[0028] (2) Dissolve TsCl (p-toluenesulfonic acid chloride) in 40ml CH 2 Cl 2 , use a dropping funnel to drop into the mixed solution prepared in the step (1), wherein TsCl and PEG n The molar ratio is 2:1, react at 25°C for 12 hours, the solution turns reddish brown and precipitates form, after filtration, the filtrate is distilled under reduced pressure, and the distillation product is dissolved in 40ml tetrahydrofuran (THF) and precipitated in 100ml ether; remove the upper layer In the clear night, place ...

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Abstract

The invention discloses a triblock copolymer polyethyleneimine (PEI)-polyethylene glycol (PEG)-PEI, belonging to the field of gene drug carriers. The triblock copolymer PEI-PEG-PEI has the structural formula as shown in the specifications. A PEI-PEG copolymer synthesized by the technical scheme of the invention has the characteristics of high transfection efficiency and low cytotoxicity, and has a wide application prospect.

Description

technical field [0001] The invention belongs to the field of gene drug carriers, and more specifically relates to a triblock copolymer PEI-PEG-PEI. Background technique [0002] A safe and effective gene carrier is a necessary condition for the realization of gene therapy. Since the cationic polymer is easy to synthesize and has no immunogenicity, it can easily form a tight supramolecular polymer with DNA, protect DNA from nuclease degradation, and promote its Entering cells, thus becoming an important type of non-viral gene vectors; however, cationic polymer gene vectors have charge-related toxicity to cells, and the transfection efficiency is lower than that of viral vectors, which has become a bottleneck limiting its application. [0003] Among the currently applied polymeric cationic carriers, polyethyleneimine (PEI) exhibits high transfection efficiency both in vivo and in vitro. Every two carbon atoms in the repeating monomer of PEI are connected to nitrogen-containin...

Claims

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Application Information

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IPC IPC(8): C08G73/02A61K47/34A61K48/00
Inventor 方剑群
Owner 方剑群
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