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Drug carrier based on sulfonium lipidosome structure and preparation method and application of drug carrier

A use, ethyl technology, applied in the field of medicine, can solve the problems of strong biological toxicity, poor targeting specificity, low gene expression efficiency, etc.

Active Publication Date: 2019-07-30
HEILONGJIANG BAYI AGRICULTURAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the chemical structure of non-viral vectors is difficult to meet various needs under biological conditions, and there are disadvantages such as poor targeting specificity, low gene expression efficiency, and strong biological toxicity during gene transfection.

Method used

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  • Drug carrier based on sulfonium lipidosome structure and preparation method and application of drug carrier
  • Drug carrier based on sulfonium lipidosome structure and preparation method and application of drug carrier
  • Drug carrier based on sulfonium lipidosome structure and preparation method and application of drug carrier

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0053] 2-(2-(2-(Nonyl)ethoxy)ethoxy)ethanol (P1)

[0054] Using the general method of P synthesis, triethylene glycol (2 mL, 14.93 mmol) was reacted with 1-iodononane (3.79 g, 14.93 mmol), sodium hydride (0.90 g, 22.5 mmol) to give P1 (1.93 g, 7.01 mmol, Yield 47%), as colorless oil; R f =0.43 (ethyl acetate-n-hexane 3:2), directly put into the next reaction.

Embodiment 2

[0056] 2-(2-(2-(Dodecyl)ethoxy)ethoxy)ethanol (P2)

[0057] Using the general method of P synthesis, triethylene glycol (2 mL, 14.93 mmol) was reacted with 1-iodododecane (4.42 g, 14.93 mmol), sodium hydride (0.90 g, 22.5 mmol) to give P2 (1.89 g, 5.95 mmol , yield 40%), as a colorless oil; R f =0.41 (ethyl acetate-n-hexane 3:2), directly put into the next reaction.

Embodiment 3

[0059] 2-(2-(2-(Hexadecyl)ethoxy)ethoxy)ethanol (P3)

[0060] Using the general method of P synthesis, triethylene glycol (2 mL, 14.93 mmol) was reacted with 1-iodohexadecane (5.26 g, 14.93 mmol), sodium hydride (0.90 g, 22.5 mmol) to give P3 (1.98 g, 5.52 mmol) , yield 37%), as a colorless oil; R f =0.38 (ethyl acetate-n-hexane 3:2), directly put into the next reaction.

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Abstract

The invention relates to the technical field of medicine, in particular to a sulfonium compound shown as a general formula (A), and discloses a preparation method of the compound. The compound is poly-condensed with genes to form a nanometer compound with the particle size of 100-300 nm and Zeta potential of +20-+40. The gene loading capability of the sulfonium compound enables the sulfonium compound to have potential application in gene transfer.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a class of sulfonium compounds, a preparation method of the compound and its use as a gene carrier. Background technique [0002] Gene therapy is a new method for human to treat diseases. It introduces therapeutic genes into diseased cells or tissues to replace or repair the defects of disease-causing genes, so as to achieve the purpose of treating diseases. Safe and effective gene delivery is a key step in gene therapy, and gene delivery vector is an important means of gene delivery. Gene vectors are mainly divided into two categories: viral vectors (Viral Vectors) and non-viral vectors (Non-viral Vectors). At present, more than 70% of clinically used vectors are viral vectors, such as adenovirus, adeno-associated virus, retroviral vector, herpes virus and pox virus. Although viral vectors have been successfully used in gene therapy with high transfection efficiency, they can...

Claims

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Application Information

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IPC IPC(8): C07D333/46C07D335/02A61K9/14A61K47/22A61K48/00
CPCC07D333/46C07D335/02A61K9/145A61K48/0008
Inventor 李婧申贵男张莹
Owner HEILONGJIANG BAYI AGRICULTURAL UNIVERSITY
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