Polyoxyalkylene Lipid Conjugates for Low-Immunogenic Stealth LNPs
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Solution Overview
Problem
Existing polyethylene oxide (PEO) based lipids used in lipid nanoparticles face issues with immune response, leading to the formation of anti-PEO antibodies, which compromise the 'stealth effect' and cause allergic reactions, while also having poor storage stability.
Innovation Solution
Development of polyoxyalkylene based compounds with a polyoxyalkylene unit different from PEO, featuring a linker unit and specific end groups, which reduce immunogenic potential and enhance storage stability.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If polyethylene oxide (PEO) based lipids are used in lipid nanoparticles, then the 'stealth effect' is achieved to avoid recognition by the reticuloendothelial system, but immune response occurs leading to formation of anti-PEO antibodies and allergic reactions
Solution Approach 1:
The patent modifies the chemical structure of the polyoxyalkylene group by changing the type of oxide units incorporated (including ethylene oxide, propylene oxide, and other alkylene oxides) and their ratios, thereby altering the physical and chemical parameters of the lipid molecule to reduce immunogenicity while preserving the stealth effect
Solution Approach 2:
The patent creates composite polyoxyalkylene structures by combining multiple types of oxide units (ethylene oxide, propylene oxide, and other alkylene oxides) within the same polyoxyalkylene group, resulting in a multifunctional lipid that provides both stealth properties and reduced immunogenicity
2Reliability
If polyethylene oxide (PEO) based lipids are used in lipid nanoparticles, then the 'stealth effect' is achieved, but storage stability is poor
Solution Approach 1:
The patent changes the compositional parameters of the polyoxyalkylene group by incorporating different types of oxide units and adjusting their ratios, which modifies the chemical stability and physical properties of the lipid, thereby improving storage stability while maintaining the stealth effect
Data Source
AI summary
The present invention refers to polyoxyalkylene based compounds and their manufacturing method as well as compositions including at least one polyoxyalkylene based compound and at least one active agent. Furthermore, the present invention refers to the manufacture of the compositions of the present invention as well as their use for the treatment of an illness in mammals or humans.