Novel carbonyl lipids and lipid nanoparticle formulations for delivery of nucleic acids

By conjugating novel lipid compounds with other lipid components to form lipid nanoparticles, the degradation and cellular uptake of free RNA in plasma have been solved, achieving more efficient nucleic acid delivery and improved in vivo and in vitro stability, while reducing toxicity risks.

CN116693411BActive Publication Date: 2026-05-29ACUITAS THERAPEUTICS INC
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
ACUITAS THERAPEUTICS INC
Filing Date
2018-04-27
Publication Date
2026-05-29

AI Technical Summary

Technical Problem

In existing technologies, free RNA is sensitive to nuclease digestion in plasma and has limited ability to enter intracellular compartments, resulting in low nucleic acid delivery efficiency. Furthermore, existing lipid nanoparticles do not provide good protection and delivery effects in vivo and in vitro.

Method used

Lipid nanoparticles are formed by conjugating novel lipid compounds with neutral lipids, charged lipids, steroids, and polymers to enhance the protection and delivery capabilities of nucleic acids, improve their stability in vivo and in vitro, and increase their cellular uptake efficiency.

Benefits of technology

It improves the efficiency of in vitro and in vivo nucleic acid delivery, enhances the protection of nucleic acids, provides a higher therapeutic index, and reduces the risk of toxicity to patients.

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Abstract

Provided are compounds having one of the following structures (I) or (II): or a pharmaceutically acceptable salt, tautomer, or stereoisomer thereof, wherein R3a, R3b, L1, L2, G1a, G1b, G2a, G2b, and G3 are as defined herein. Also provided are uses of the compounds as components of lipid nanoparticle formulations for the delivery of therapeutic agents, compositions comprising the compounds, and methods of using and making the same.
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