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Polyamino acid segmented copolymer serving as siRAN carrier and preparation method as well as composite particle

A technology of block copolymer and polyamino acid, applied in the field of polymer, can solve the problems of insufficient concentration of charge density and weak ability to compound genetic material, and achieve the effects of reducing toxicity, good biocompatibility, and strong compounding ability

Active Publication Date: 2014-05-21
长春金传科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the carrier needs a higher mass ratio to achieve the best transfection effect, which shows that the charge density of the linear polyaspartic acid grafted polyethyleneimine copolymer is not concentrated enough, and the ability to compound gene substances is weak

Method used

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  • Polyamino acid segmented copolymer serving as siRAN carrier and preparation method as well as composite particle
  • Polyamino acid segmented copolymer serving as siRAN carrier and preparation method as well as composite particle
  • Polyamino acid segmented copolymer serving as siRAN carrier and preparation method as well as composite particle

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preparation example Construction

[0048] The invention also discloses a preparation method of a polyamino acid block copolymer used as an siRNA carrier, comprising the following steps:

[0049] (A) Under the protection of inert gas, β-benzyl-L-aspartic acid-N-carboxylic acid anhydride reacts with branched polyethyleneimine in an organic solvent to obtain an intermediate product;

[0050] (B) reacting the intermediate product obtained in step (A) with polyethyleneimine under the action of a catalyst to obtain a polyamino acid block copolymer used as an siRNA carrier;

[0051] The polyamino acid block copolymer used as siRNA carrier is shown in formula (I):

[0052]

[0053] R is selected from one of the structures shown in formula (11) ~ formula (14):

[0054]

[0055]

[0056] The NH- of the R is connected to the C atom in the formula (I);

[0057] Ph is

[0058] where x 1 ,y 1 ,z 1 ,x 2 ,y 2 ,z 2 ,x 3 ,y 3 ,z 3 , m, n, a, b and c are degrees of aggregation, x 1 ,y 1 ,x 3 ,y 3 ,z 3 ...

Embodiment 1

[0070] Under anhydrous and oxygen-free conditions, add 4.7 g of β-benzyl-L-aspartic acid-N-carboxylic acid anhydride to a dry reaction ampoule, fill it with nitrogen protection, and add 300 mL of anhydrous N',N' - Dimethylformamide, stirred to dissolve.

[0071] 19 mL of branched polyethyleneimine with a weight average molecular weight of 600 was dissolved in anhydrous chloroform to obtain a polyethyleneimine / chloroform solution with a concentration of 0.01 mmol / mL. Take 19 mL of polyethyleneimine / chloroform solution and add it into the reaction ampoule, and stir the reaction at 30° C. for 72 hours under temperature control. After the reaction is completed, settle in 3000 mL of ether, filter and dry the filter cake to obtain poly-L-aspartic acid-β-benzyl ester with a molecular weight of 21000.

Embodiment 2

[0073] Under anhydrous and oxygen-free conditions, add 4.7 g of β-benzyl-L-aspartic acid-N-carboxylic acid anhydride to a dry reaction ampoule, fill it with nitrogen protection, and add 300 mL of anhydrous N',N' - Dimethylformamide, stirred to dissolve.

[0074]3.8 mL of branched polyethyleneimine with a weight average molecular weight of 600 was dissolved in anhydrous chloroform to obtain a polyethyleneimine / chloroform solution with a concentration of 0.01 mmol / mL. Take 19 mL of polyethyleneimine / chloroform solution and add it into the reaction ampoule, and stir the reaction at 30° C. for 72 hours under temperature control. After completion of the reaction, settle in 3000 mL of ether, filter and dry the filter cake to obtain poly-L-aspartic acid-β-benzyl ester with a molecular weight of 100800.

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Abstract

The invention provides a polyamino acid segmented copolymer serving as a siRAN carrier shown in a formula (I). A preparation method for the polyamino acid segmented copolymer comprises the following steps of: enabling beta-benzyl-L-aspartic acid-N-carboxylic acid anhydride to react with cladodification polyethyleneimine in an organic solvent under the protection of inert gas to obtain an intermediate product; enabling the obtained intermediate product to react with polyethyleneimine under the action of a catalytic agent to obtain the polyamino acid segmented copolymer serving as the siRAN carrier. The invention provides a composite particle which comprises the polyamino acid segmented copolymer serving as the siRAN carrier and siRNA; and the siRNA is the Luc siRNA of silent luciferase. The polyamino acid segmented copolymer serving as the siRAN carrier provided by the invention has concentrated electric charge density, strong composite capacity and good biological compatibility; and the toxicity of the polyamino acid segmented copolymer is effectively reduced.

Description

technical field [0001] The invention relates to the field of high polymers, in particular to a polyamino acid block copolymer used as an siRNA carrier, a preparation method and composite particles. Background technique [0002] With the development of modern biotechnology and the continuous improvement of the human gene pool, it has gradually become possible for humans to understand the root causes of certain diseases at the molecular level, providing a theoretical basis for gene therapy. In practice, how to obtain safe and effective gene carriers has increasingly become a bottleneck problem restricting the clinical application of gene therapy. The use of viral vectors to mediate gene transfer is the most widely used method in gene therapy, including retroviruses, adenoviruses, adeno-associated viruses, herpes simplex virus, vaccinia virus and other vectors. However, there are great safety hazards in the clinical application of viral vectors, which caused the first patient ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C08G81/00C08G69/08C12N15/87
Inventor 田华雨董璇陈学思林琳
Owner 长春金传科技有限公司
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