Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Cationic liposome with high gene transfection efficiency and preparation and application thereof

A technology of cationic lipids and amino groups, which is applied in the directions of organic chemistry, the use of microcapsules, and other methods of inserting foreign genetic materials, can solve the problems of complex preparation methods, low transfection efficiency, unstable prices, etc., and achieves simple preparation methods. , Improve transfection efficiency and low toxicity

Pending Publication Date: 2022-03-15
HUAZHONG UNIV OF SCI & TECH
View PDF0 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The invention solves the key technical problems of existing gene delivery vectors (including viral vectors and non-viral vectors), immunogenicity, systemic toxicity, complex preparation methods, low transfection efficiency, instability and high price.

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Cationic liposome with high gene transfection efficiency and preparation and application thereof
  • Cationic liposome with high gene transfection efficiency and preparation and application thereof
  • Cationic liposome with high gene transfection efficiency and preparation and application thereof

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0055] A method for preparing an amphiphilic cationic lipid material of the present invention comprises the following steps:

[0056] (1) Reflux the compound containing monosulfide bond, disulfide bond, disulfide bond, diselenide bond, monoselenide bond or diselenide bond in acetyl chloride to obtain product A;

[0057] (2) Dissolve vitamin E, cholesterol, cis-9-octadecenol, catalyst 4-dimethylaminopyridine and the product A obtained in step (1) in an organic solvent, and stir and react at 50°C-80°C for 12h -36h, obtain product B;

[0058] (3) The product B obtained in step (2), 3-amino-1,2-propanediol, catalyst 4-dimethylaminopyridine and catalyst 1-(3-dimethylaminopropyl)-3-ethyl carbon Diimine hydrochloride was dissolved in an organic solvent, stirred and reacted at 25°C-37°C for 16h-24h to obtain product C;

[0059] (4) dissolving the product C obtained in step (3) in an organic solvent, adding trifluoroacetic acid equal to the volume of the organic solvent, stirring and...

Embodiment 1

[0082] This embodiment provides a method for preparing a novel amphiphilic cationic lipid material sensitive to esterase, which is synthesized through the following steps:

[0083](1) Synthesis of VE-COOH: 4.3g of vitamin E (VE), 1.5g of succinic anhydride (SA) and 3.15g of triethylamine were weighed into a 100mL round bottom flask, and 50mL of dichloromethane was added. After stirring and dissolving at 70°C, the reflux reaction was continued for 24h. After the reaction, add 50 mL of deionized water for extraction three times, dry the organic layer with anhydrous sodium sulfate overnight, filter, and remove the organic solvent by rotary evaporation. The obtained oil is dissolved in three times the amount of n-hexane at 60°C, and then gradually cooled to room temperature , and then recrystallized overnight at 4°C. After filtration, a white powdery solid was obtained, and the obtained white powder was vacuum-dried overnight at 40° C. to remove residual organic solvents to obtai...

Embodiment 2

[0097] This example provides a method for preparing a novel amphiphilic cationic lipid material with redox sensitivity, which is synthesized through the following steps:

[0098] (1) Synthesis of 2,2'-thiodiacetic anhydride: Weigh 3.0 g of 2,2'-thiodiacetic acid into a 50 mL round-bottomed flask, and add 25 mL of acetic anhydride. After reflux reaction at 65°C for 4 hours, distill under reduced pressure to remove acetic anhydride, acetic acid, etc.; add an appropriate amount of ether, and repeat the rotary evaporation 2-3 times to obtain a white solid powder, which is dried in vacuum at 40°C overnight to obtain 2,2'-sulfur Substitute diacetic anhydride, the productive rate is 98.7%.

[0099] (2) Synthesis of VE-S-COOH: Weigh 4.3g of vitamin E (VE), 1.98g of 2,2-thiodiacetic anhydride and 1.12g of 4-dimethylaminopyridine in a 100mL round bottom flask, add 50mL dichloromethane. After stirring and dissolving at 70°C, the reflux reaction was continued for 36h. After the reactio...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

The invention relates to a cationic liposome with high gene transfection efficiency as well as preparation and application thereof, and belongs to the technical field of chemical drugs. The cationic lipid material comprises a hydrophobic end, a chemical sensitive area, a connecting arm and a hydrophilic end, the hydrophobic end, the chemical sensitive area, the connecting arm and the hydrophilic end are connected in sequence; the chemical sensitive area comprises a chemical sensitive bond, and the chemical sensitive bond is a chemical bond which can be broken under an oxidation-reduction condition, an enzyme catalysis condition or an acidic pH condition. The cationic lipid material can be self-assembled to obtain the cationic liposome with a bilayer structure, the cationic liposome is small in particle size, is positively charged, and can form a stable nano-composite with a negatively charged gene drug, and the composite can be effectively taken by cells, enters the cells and is stably transfected in the cells, and has very high transfection efficiency.

Description

technical field [0001] The invention belongs to the technical field of chemical medicines, and more specifically relates to a cationic liposome with high gene transfection efficiency and its preparation and application. Background technique [0002] With the deepening of people's understanding of the pathogenesis of diseases at the cellular level, gene therapy has increasingly become a research hotspot for scientists. Searching for safe and effective gene delivery vectors has attracted more and more attention. [0003] Current research shows that gene delivery vectors are mainly divided into two categories: viral vectors and non-viral vectors. Viral vectors have certain advantages in gene delivery due to their high transfection efficiency and targeting effect on most cells. However, due to the immunogenicity of the viral vector, it can cause a series of immune responses in the body, and the viral genes contained in it may undergo gene recombination or complementation in th...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
IPC IPC(8): C07D405/14C12N15/88
CPCC07D405/14C12N15/88
Inventor 张志平余育林
Owner HUAZHONG UNIV OF SCI & TECH
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com