Reverse Micelle Nucleic Acid Delivery System
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Solution Overview
Problem
Current nucleic acid delivery systems face challenges such as instability in biological fluids, poor intracellular penetration, and low bioavailability, which limits their therapeutic effectiveness, particularly for genetic and inflammatory diseases, due to instability and inefficient delivery across cellular membranes.
Innovation Solution
Development of reverse micelle systems comprising sterols, acylglycerols, phospholipids, or sphingolipids, and nucleic acids, which form stable microemulsions that can cross mucosal and cellular membranes, enhancing the bioavailability and stability of nucleic acids for therapeutic delivery.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If nucleic acids are administered directly, then they can be delivered to target sites, but they display poor intracellular penetration and low bioavailability
Solution Approach 1:
The patent employs reverse micelles as intermediary carriers to facilitate nucleic acid delivery. These micelles consist of amphiphilic molecules with hydrophilic heads and hydrophobic tails, forming structures that can encapsulate nucleic acids in their core while interacting with cellular membranes, thereby mediating the transfer of nucleic acids across biological barriers and into cells
Solution Approach 2:
The patent modifies the physical and chemical parameters of nucleic acids by incorporating them into reverse micelle structures. This changes their solubility, stability, and membrane interaction properties, enabling them to cross cellular membranes and achieve intracellular delivery that is not possible in their native state
2Reliability
If nucleic acids are administered in biological fluids, then they can reach target sites, but they are unstable and display low bioavailability
Solution Approach 1:
Reverse micelles serve as protective intermediaries that shield nucleic acids from degradation by nucleases and other enzymes in biological fluids. The micellar structure provides a stable environment that maintains nucleic acid integrity during transport through the bloodstream to target sites
Solution Approach 2:
The reverse micelle structure provides a flexible protective shell around the nucleic acid core. This shell consists of the amphiphilic molecule arrangement that creates a stable interface between the hydrophilic exterior (facing biological fluids) and the hydrophobic core (protecting the nucleic acid), thereby enhancing stability while maintaining bioavailability
3Quantity of substance
If high doses of nucleic acid are delivered, then therapeutic activity can be achieved, but stability is insufficient without proper formulation
Solution Approach 1:
The patent creates a composite material system consisting of nucleic acids combined with amphiphilic molecules that self-assemble into reverse micelles. This composite structure allows high loading of nucleic acids in the hydrophobic core while the hydrophilic exterior maintains stability in aqueous biological environments, achieving both high dose delivery and formulation stability
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 reverse micelle system effectively increases the stability and bioavailability of nucleic acids, allowing for efficient gene expression modulation and therapeutic activity at lower doses, with improved absorption and distribution within the body, including across the blood-brain barrier.
Implementation Method 1
reverse micelle systems comprising sterols, acylglycerols, phospholipids, or sphingolipids, and nucleic acids, which form stable microemulsions
Implementation Method 2
The reverse micelle system is able to cross mucosa and cellular membranes
Data Source
AI summary
The present invention relates to reverse micelle system based on sterols, acylglycerols, phospholipids or sphingolipids and nucleic acids. The reverse micelle system of the invention is able to cross mucosa and cellular membranes. It thus allows vectorization of nucleic acids to target sites. It is advantageously useful in the pharmaceutical and dietetic fields.