Lecithin Multi-Lamellar Vesicles for Oral Delivery
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Solution Overview
Problem
Current liposome technologies are not well-suited for oral delivery due to their instability in the harsh acidic environment of the stomach and the digestive enzymes in the small intestine, which leads to the destruction of liposomes and their contents.
Innovation Solution
Development of novel multi-lamellar vesicles comprising lecithin, which are greater than 3 μm in size, providing a stable delivery system for oral cargo. These vesicles are prepared by mixing lecithin in a buffer until fully dispersed, and can incorporate a variety of cargo, including hydrophilic and hydrophobic molecules.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If conventional liposomes are used for oral delivery, then encapsulation of hydrophilic and hydrophobic cargo is achieved, but stability in the harsh acidic environment of the stomach and digestive enzymes is lost
Solution Approach 1:
The patent changes the physical parameters of the vesicles by creating multi-lamellar structures with thicker effective membrane barriers and larger sizes (>3 μm). This structural parameter change provides enhanced resistance to enzymatic degradation and acidic environments, resolving the stability issue while maintaining encapsulation capability
Solution Approach 2:
The invention uses composite phospholipid compositions including multiple types of phospholipids (PC, PE, PS, PI) in specific ratios, creating a composite membrane structure that is more resistant to digestive enzymes and acid than conventional single-component liposomes, thereby improving reliability in the digestive system
2Quantity of substance
If small unilamellar vesicles (SUVs) are used, then encapsulation efficiency is improved, but long-term stability without stabilizers is compromised
Solution Approach 1:
The patent creates multi-lamellar vesicles with nested concentric bilayers, where multiple membrane layers provide both encapsulation capacity and structural stability. The nested structure allows high encapsulation efficiency while the multiple layers provide long-term stability without requiring additional stabilizers
Solution Approach 2:
The invention uses flexible phospholipid bilayer films arranged in multiple concentric layers. These flexible films can adapt to environmental changes while maintaining structural integrity, providing both high encapsulation efficiency and long-term stability
3Length of moving object
If high energy processes like sonication or microfluidization are used to produce small vesicles, then vesicle size is reduced for better circulation, but structural integrity and simplicity of the system is compromised
Solution Approach 1:
Instead of using high-energy processes to break down large vesicles into small ones, the invention inverts the approach by allowing spontaneous self-assembly of phospholipids to directly form multi-lamellar vesicles of the desired size range. This gentle self-assembly process preserves structural integrity while achieving the required vesicle dimensions for oral delivery
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 large multi-lamellar vesicles demonstrate enhanced stability and effectiveness for oral delivery, capable of maintaining their structure and integrity through the digestive system, thereby ensuring effective encapsulation and delivery of cargo.
Implementation Method 1
When exposed to either hydrophobic or hydrophilic environments, these molecules associate with each other such that hydrophilic or water-loving regions associate with other such regions, and hydrophobic or water-hating regions associate with other such regions. This molecular 'phase separation' is the driving force for self-assembly and eventual supramolecular structure formation.
Implementation Method 2
Phospholipids are amphipathic (or amphiphilic) molecules which contain hydrophobic and hydrophilic parts. When exposed to either hydrophobic or hydrophilic environments, these molecules associate with each other such that hydrophilic or water-loving regions associate with other such regions, and hydrophobic or water-hating regions associate with other such regions.
Implementation Method 3
The large multi-lamellar vesicles demonstrate enhanced stability and effectiveness for oral delivery, capable of maintaining their structure and integrity through the digestive system
Data Source
AI summary
Giant multi-lamellar vesicles (GMVs) comprising lecithin are provided which are at least about 3 μm in size. Methods for preparing the GMVs, and for preparing large unilamellar vesicles (LUVs) from the GMVs, are provided, as well as methods for encapsulating cargo within the GMVs and LUVs. The present vesicles are useful for the oral delivery of encapsulated cargo.