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Lysine grafted polyethyleneimine cation gene vector as well as preparation method and application thereof

A technology of polyethyleneimine cation and polyethyleneimine, applied in the field of lysine-grafted polyethyleneimine cation gene carrier and its preparation, can solve the problems of limited application and severe cytotoxicity

Active Publication Date: 2022-02-15
CHANGCHUN INST OF APPLIED CHEMISTRY - CHINESE ACAD OF SCI
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Although PEI25k has high transfection efficiency, it has severe cytotoxicity, which limits its clinical application

Method used

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  • Lysine grafted polyethyleneimine cation gene vector as well as preparation method and application thereof
  • Lysine grafted polyethyleneimine cation gene vector as well as preparation method and application thereof
  • Lysine grafted polyethyleneimine cation gene vector as well as preparation method and application thereof

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preparation example Construction

[0028] The present invention provides the preparation method of above-mentioned cationic gene carrier, comprises the following steps:

[0029] S1) mixing EDC·HCl and HOBT with p-toluenesulfonyl and tert-butoxycarbonyl double-protected lysine in an organic solvent for activation;

[0030] S2) Mixing the activated solution in step S1) with an aqueous solution of hyperbranched polyethyleneimine for reaction, followed by dialysis and freeze-drying to obtain an intermediate product;

[0031] S3) Use trifluoroacetic acid to deprotect the intermediate product obtained in step S2), and then settle in anhydrous ether. The product is vacuum-dried, dialyzed, and freeze-dried to obtain the cationic gene carrier PEI-Lys (Tos).

[0032] Preferably in the present invention, the organic solvent is DMF, DMSO, dichloromethane or trichloromethane.

[0033] Preferably in the present invention, the activation temperature is 20-40°C, more preferably 30°C.

[0034] Preferably in the present invent...

Embodiment 1PE

[0054] The synthesis of embodiment 1PEI1.8k-Lys (Tos)

[0055]

[0056] Dissolve small molecular weight polyethyleneimine PEI1.8k and Boc-Lys(TOS)-OH in DMF, then add HOBT and EDCI to it, react at room temperature for 72 hours, then dialyze the reacted solution with 2000 dialysis bag, freeze-dry, The freeze-dried sample was dissolved in trifluoroacetic acid, reacted at room temperature for 4 hours, diethyl ether was settled, vacuum spin-dried, dissolved in deionized water, then dialyzed in 2000 dialysis bags, freeze-dried to obtain hyperbranched polyethyleneimine (PEI) grafted Branch p-tosyl-protected lysine (PEI 1.8k -Lys(Tos)).

[0057] According to the above method, 3 different grafting ratios of PEI grafted with tosyl-protected lysine (Lys(Tos)) were prepared, and the grafting ratios are listed in Table 1.

[0058] The corresponding relation of the mol ratio of table 1 raw material and product molecular weight

[0059]

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Abstract

The invention provides a lysine grafted polyethyleneimine cationic gene vector. The lysine grafted polyethyleneimine cationic gene vector comprises hyperbranched polyethyleneimine and lysine which is grafted on the hyperbranched polyethyleneimine and is protected by p-toluenesulfonyl. In order to realize high-efficiency delivery of a gene vector to a gene, polyethyleneimine with small molecular weight is modified, and lysine protected by p-toluenesulfonyl is grafted on the polyethyleneimine. According to the invention, three PEI-Lys (Tos) carriers with different grafting ratios (1: 5; 1: 10; 1: 15) are prepared. Through comparison, the grafting ratio (1: 10) with the best transfection performance is screened for other subsequent evaluation characterization. Experimental results show that the PEI-Lys (Tos) cationic carrier prepared through modification design has higher transfection efficiency and lower cytotoxicity, and has a huge application prospect in the fields of gene carrier design and tumor resistance.

Description

technical field [0001] The invention relates to the technical field of biomedical new materials, in particular to a lysine-grafted polyethyleneimine cationic gene carrier and its preparation method and application. Background technique [0002] At present, there are many methods for tumor treatment. Traditional therapies such as radiotherapy, chemotherapy, and surgical resection have disadvantages such as large side effects and easy recurrence; while some emerging therapies, such as phototherapy and immunotherapy, also have disadvantages such as low response rate and large toxic and side effects. Gene therapy has been recognized as an important means of cancer treatment because it can correct pathological defects at the gene level and thereby cure cancer. Gene delivery in vitro and in vivo is inseparable from gene carriers. When the gene carrier carries the therapeutic gene for transport in the body, the delivery system will encounter many obstacles in the body. Among gene...

Claims

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Application Information

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IPC IPC(8): C08G73/02C12N15/87
CPCC08G73/0206C12N15/87Y02P20/55
Inventor 田华雨林琳郭兆培胡莹莹陈学思
Owner CHANGCHUN INST OF APPLIED CHEMISTRY - CHINESE ACAD OF SCI
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