Boron Compounds in Lipid Particles for Nucleic Acid Delivery
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Solution Overview
Problem
Current methods for delivering nucleic acids to cells or animals are often inefficient and limited, hindering disease treatment and gene therapy applications.
Innovation Solution
Development of boron compounds, specifically those of Formula (I), which are incorporated into lipid particles and lipoplexes to facilitate efficient delivery of nucleic acids. These compounds react with lipid particle components to form covalent bonds, enhancing delivery efficacy.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Productivity
If conventional methods are used for delivering nucleic acids, then the delivery process is simple, but the delivery efficiency is low
Solution Approach 1:
The patent employs composite lipid particles containing boron compounds combined with nucleic acids to create a multifunctional delivery system. The boron compounds form covalent bonds with lipid components, creating a stable composite structure that enhances delivery efficiency while maintaining manageable complexity through systematic formulation.
Solution Approach 2:
Boron compounds serve as intermediary agents that facilitate the interaction between lipid particles and nucleic acids. The boron compounds react with diol-containing lipids to form boronate esters, creating a bridging structure that stabilizes the lipoplex and improves nucleic acid delivery efficiency.
2Reliability
If boron compounds are incorporated into lipid particles to form covalent bonds, then delivery efficacy is enhanced, but the manufacturing process becomes more complex
Solution Approach 1:
The boron compounds are pre-incorporated into the lipid particle formulation before nucleic acid addition. This preliminary incorporation allows the boron-lipid covalent bonds to form in advance, creating a stable delivery vehicle that simplifies the overall manufacturing process by eliminating the need for post-assembly bond formation.
Solution Approach 2:
The patent utilizes changes in chemical parameters, specifically the formation of boronate ester bonds between boron compounds and diol-containing lipids. This chemical parameter change creates stable covalent linkages that enhance delivery efficacy while the reaction conditions are optimized to maintain manufacturing feasibility.
Applied Scientific Principles
This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.
Function Achieved in This Case
The use of boron compounds in lipid particles and lipoplexes significantly improves the delivery of nucleic acids, potentially leading to effective disease treatment, gene silencing, and immune response induction.
Implementation Method 1
the boron compound reacts with a lipid particle component in the lipid particle to form one or more covalent bonds between the boron compound and the lipid particle component
Data Source
AI summary
Some embodiments of the invention include inventive compounds (e.g., boron compounds of Formula (I)), inventive lipid particles, and inventive lipoplexes. Other embodiments include compositions (e.g., pharmaceutical compositions) comprising the inventive compound, inventive lipid particles, or inventive lipoplexes. Some embodiments include methods of using the inventive lipoplexes (e.g., in compositions or in pharmaceutical compositions) for administering, treating disease, inducing an immune response, and combinations thereof. Further embodiments include methods for making the inventive compounds. Additional embodiments of the invention are also discussed herein.