POEGMA-based lipid nanoparticles

JP2024541924A5Pending Publication Date: 2025-10-31DUKE UNIV
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Patent Information

Application Number
JP2024524728
Authority / Receiving Office
JP · JP
Patent Type
Applications
Current Assignee / Owner
Priority Date
2021-10-25
Filing Date
2022-10-25
Publication Date
2025-10-31

AI Technical Summary

Technical Problem

Lipid nanoparticles (LNPs) with PEG coating face limitations such as immunogenicity, allergic side effects, and enhanced clearance by the reticuloendothelial system (RES), leading to clinical trial terminations and withdrawal of therapeutics due to PEG intolerance, particularly in mRNA vaccines like the Pfizer-BioNTech COVID-19 vaccine.

Method used

Development of lipid nanoparticles containing less than 10 mol% of a POEGMA-lipid conjugate with a number average molecular weight of less than 100 kDa, which replaces PEG for stealth properties, reducing immunogenicity and enhancing biocompatibility.

Benefits of technology

The POEGMA-lipid conjugates provide efficient encapsulation of therapeutic agents like mRNA with over 85% encapsulation efficiency, protect mRNA from RNases, and demonstrate improved in vivo delivery potential, outperforming Moderna biosimilar formulations in reporter mRNA expression assays.

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Abstract

Disclosed herein are lipid nanoparticles comprising POEGMA-lipid conjugates that can effectively encapsulate and deliver therapeutic agents without the immunological consequences incurred by their PEG-based counterparts. Exemplary lipid nanoparticles include ionizable lipids, phospholipids, sterols, POEGMA-lipid conjugates, and therapeutic agents. Also disclosed herein are pharmaceutical compositions comprising POEGMA-based lipid nanoparticles, methods of treating diseases or disorders, and methods of delivering therapeutic agents to cells.
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