Ionizable lipids and uses thereof

By introducing pyrazole ring structures and ester groups into ionizable lipid compounds, the resulting lipid nanoparticles improve the delivery and encapsulation efficiency of nucleic acids, solving the problems of nucleic acid degradation and low delivery efficiency in vivo, and achieving improved stability and therapeutic efficacy of nucleic acid therapeutic agents.

CN122094940APending Publication Date: 2026-05-26KOREA GREEN CROSS CORP
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
KOREA GREEN CROSS CORP
Filing Date
2024-10-23
Publication Date
2026-05-26

AI Technical Summary

Technical Problem

Existing technologies struggle to effectively prevent nucleic acids from being degraded by enzymes in vivo and to deliver them to target cells, especially due to their negative charge and large molecular weight, which result in low delivery efficiency.

Method used

A novel ionizable lipid compound was synthesized by introducing a pyrazole ring structure into the head of the ionizable lipid and adding ester or branched ester groups to the terminal hydrocarbon chain to form lipid nanoparticles (LNPs) with excellent cell delivery efficiency. Phospholipids, cholesterol and PEG-lipids were then combined to stabilize and disperse nucleic acids.

Benefits of technology

This improved the delivery and encapsulation efficiency of nucleic acids, enhancing the in vivo stability and therapeutic efficacy of nucleic acid therapeutic agents.

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Abstract

This invention relates to a novel ionizable lipid compound or a salt thereof represented by formula (I), and lipid nanoparticles comprising the ionizable lipid compound or a salt thereof. Lipid nanoparticles comprising the novel ionizable lipid compound according to the invention exhibit excellent nucleic acid encapsulation efficiency and high cellular delivery efficiency for nucleic acids.
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Citation Information

Patent Citations

  • Cationic sulfonamide amino lipids and amphiphilic zwitterionic amino lipids

    US20200140378A1