Ionizable lipids for use in lipid nanoparticles

AU2025211367A1Pending Publication Date: 2026-09-10MERCK PATENT GMBH
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Patent Information

Application Number
AU2025211367
Authority / Receiving Office
AU · AU
Patent Type
Applications
Current Assignee / Owner
Priority Date
2024-01-26
Filing Date
2025-01-24
Publication Date
2026-09-10

AI Technical Summary

Technical Problem

Current lipid nanoparticles used for nucleic acid delivery, such as mRNA therapeutics, face challenges including rapid aggregation, instability at room temperature, and inefficiencies in cellular uptake and delivery, particularly for chronic conditions like cystic fibrosis, necessitating improved ionizable lipids with enhanced pharmacokinetic properties and reduced toxicity.

Method used

Development of novel ionizable lipids, represented by compounds of formula (I) and (la), which form lipid nanoparticles that optimize nucleic acid delivery by providing improved stability, cellular uptake, and reduced toxicity, allowing for efficient delivery to various tissues and organs, and are designed using machine learning techniques to enhance properties.

Benefits of technology

The novel ionizable lipids achieve stable formulations at room temperature, enhance cellular uptake, and reduce toxicity, enabling effective nucleic acid delivery with a favorable therapeutic index, suitable for both systemic and local administration.

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Abstract

The present invention relates to ionizable lipids for use in lipid nanoparticles, lipid nanoparticle formulations comprising these ionizable lipids, alone or in combination with other lipids and / or polymers. The lipid nanoparticles formulations may be formulated with nucleic acids for their delivery to target tissues after administration, in particular after parenteral administration such as intravenous, intramuscular, subcutaneous or intratumoral administration.
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