Reverse Micelle Encapsulation of Nucleic Acids in Biodegradable Polymers
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Solution Overview
Problem
Current methods for encapsulating charged hydrophilic agents like nucleic acids in biodegradable polymers face challenges such as low encapsulation yield, low drug-to-carrier weight ratios, and irreproducibility, often requiring high shear emulsification, which leads to product losses and inefficiencies.
Innovation Solution
A method using reverse micelles to efficiently encapsulate therapeutic agents by forming non-toxic reverse micelles that trap hydrophilic agents and disperse them into a nanosuspension, facilitating their incorporation into the hydrophobic core of biodegradable polymers, improving encapsulation yield and reproducibility without the need for damaging emulsification techniques.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Volume of moving object
If high shear emulsification is used to encapsulate hydrophilic agents in biodegradable polymers, then nanoparticle size is achieved, but product losses increase and encapsulation yield decreases
Solution Approach 1:
The patent uses reverse micelles as an intermediary structure to encapsulate hydrophilic therapeutic agents before incorporating them into the hydrophobic polymer matrix. The reverse micelles act as a mediator that protects the hydrophilic agents during the encapsulation process, eliminating the need for high shear emulsification and reducing product losses while achieving the desired nanoparticle size.
2Stability of the object's composition
If conventional encapsulation methods are used for charged hydrophilic agents, then polymer matrix formation is achieved, but encapsulation yield and drug-to-carrier weight ratios are low
Solution Approach 1:
The patent performs preliminary encapsulation of hydrophilic therapeutic agents within reverse micelles before incorporating them into the polymer matrix. This preliminary action protects the charged hydrophilic agents and ensures high encapsulation yield and optimal drug-to-carrier weight ratios while maintaining polymer matrix formation.
3Volume of moving object
If high shear emulsification is used to achieve nanoparticle size, then particle size is controlled, but reproducibility decreases
Solution Approach 1:
The patent changes the key parameter from shear rate to reverse micelle concentration and composition to control nanoparticle size. This parameter change enables precise control over particle size while significantly improving reproducibility, as reverse micelle formation is a self-organizing process that occurs under mild conditions without requiring high shear emulsification.
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
This approach enhances encapsulation efficiency, drug-to-carrier ratios, and reproducibility of nanoparticle formation, while using naturally-derived or FDA-approved components for clinically relevant drug delivery vehicles, specifically targeting cancer treatment by optimizing ligand density and stealth characteristics.
Implementation Method 1
forming non-toxic reverse micelles. These reverse micelles effectively entrap therapeutic agents, such as hydrophilic therapeutic agents, and disperse them into a nanosuspension, facilitating their incorporation into the hydrophobic core of biodegradable polymers
Data Source
AI summary
A method for encapsulating nucleic acids, particularly siRNAs, shRNAs, microRNAs, gene therapy plasmids, and other oligonucleotides in biodegradable polymers is disclosed, whereby the nucleic acids are formulated into reverse micelles composed of non-toxic and/or naturally-occurring lipids prior to nanoparticle formation by nanoprecipitation. This method can be coupled to other techniques that improve intracellular drug targeting, ultimately enhancing intracellular delivery of the aforementioned nucleic acids.