Micellar System for Targeted Active Ingredient Transport
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Solution Overview
Problem
Existing drug formulations face challenges in achieving high concentrations of diverse active ingredients with targeted and defined release profiles, particularly in providing oral administration and avoiding immune system responses.
Innovation Solution
Active ingredient compositions containing at least two types of micelles, each with a core containing an active ingredient and a shell of polyelectrolytes and/or glycerol esters, with a mean geometric diameter of 5-100 nm, allowing for targeted and controlled release of active ingredients in the gastrointestinal tract.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Quantity of substance
If high concentrations of diverse active ingredients are provided in drug formulations, then the therapeutic efficacy is improved, but the stability and controlled release profile deteriorate
Solution Approach 1:
The formulation segments diverse active ingredients into separate micellar carriers with different shell compositions. Each micelle type is optimized for specific active ingredients, allowing high concentrations of multiple ingredients to coexist stably without interfering with each other's release profiles.
Solution Approach 2:
The invention uses composite micellar structures with different shell materials (polyelectrolytes and/or glycerol esters) to create a multi-component delivery system. This composite approach allows simultaneous incorporation of diverse active ingredients while maintaining individual stability and controlled release characteristics for each ingredient type.
2Manufacturing precision
If targeted and defined release profiles are provided, then the therapeutic precision is improved, but the formulation complexity increases
Solution Approach 1:
Different micelle types are assigned different shell compositions and properties tailored to specific active ingredients and their desired release characteristics. This local optimization allows each micelle population to have a defined release profile suited to its cargo, achieving therapeutic precision without requiring a single complex formulation design.
Solution Approach 2:
The invention controls release profiles by varying micelle parameters such as shell composition (polyelectrolyte type, glycerol ester type), shell thickness, and micelle size. These parameter adjustments provide targeted release without increasing overall formulation complexity, as each parameter change directly translates to a specific release characteristic.
3Ease of operation
If micelles are administered orally, then the ease of administration is improved, but the risk of immune system response increases
Solution Approach 1:
The micelle size parameter is optimized to fall within the 5-100 nm range, which is small enough to evade immune detection by macrophages and other immune cells. This size parameter change allows oral administration to proceed without triggering significant immune responses, maintaining ease of administration while reducing harmful immune effects.
Solution Approach 2:
The polyelectrolyte and glycerol ester shell materials act as intermediaries that protect the active ingredients from immune recognition while allowing oral passage. These biocompatible shell materials mediate between the potentially immunogenic active ingredients and the immune system, enabling oral administration without triggering immune responses.
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 micelles efficiently transport active ingredients across the gastrointestinal tract, avoiding immune reactions and enabling targeted release in the small intestine, enhancing bioavailability and stability.
Implementation Method 1
artificially produced, self-agglomerating, stable micelles
Implementation Method 2
The nanoscale micelles efficiently circumvent the immune system's response
Implementation Method 3
release the active ingredient at a predetermined location (directed) and/or over a predetermined time (release profile)
Implementation Method 4
The micelles efficiently transport active ingredients across the gastrointestinal tract
Data Source
AI summary
The invention relates to a micelle-containing active ingredient composition, wherein the micelle-containing active ingredient composition contains at least two different types of micelles, and each type of micelles contains at least one polyelectrolyte selected from oligosaccharides and/or polysaccharides, and/or at least one glycerol ester selected from fatty acid glycerol esters and/or glycerol esters of wood rosins, and at least one active ingredient. The invention also relates to a method for producing such types of micelles.