Surfactant-Enhanced Phospholipid Vesicles for Lipophilic Molecule Loading
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Solution Overview
Problem
Existing methods for encapsulating lipophilic passenger molecules in nano-sized phospholipid structures face stability issues, leading to precipitation and reduced usability, especially at higher concentrations, limiting their application in pharmaceutical and cosmetic formulations.
Innovation Solution
The use of surfactants as encapsulating agents in phospholipid vesicles to enhance the encapsulation of lipophilic passenger molecules, increasing stability and preventing precipitation, with compositions containing up to 25% surfactant and less than 2% water, allowing for higher concentrations of cannabinoids and other lipophilic substances to be maintained in a stable state.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of manufacture
If aqueous-diluted formulations are used to encapsulate lipophilic passenger molecules in phospholipid particles, then the particles can be prepared and administered, but the formulations become unstable and precipitate within 1-3 days
Solution Approach 1:
The patent changes the chemical composition parameters by replacing water-based aqueous phases with organic solvent-based phases (ethanol, isopropanol, or their mixtures with surfactants). This parameter change transforms the formulation from water-based to organic-solvent-based, enabling stable encapsulation of lipophilic molecules at high concentrations without precipitation for extended periods (weeks to months).
Solution Approach 2:
The patent employs composite formulation systems combining phospholipids with organic solvents (ethanol/isopropanol) and surfactants (polysorbates, PEG esters). This composite approach creates a synergistic system where the organic solvent maintains lipophilic molecule solubility, phospholipids form the vesicular structure, and surfactants stabilize the interface, preventing precipitation while enabling high loading concentrations.
2Quantity of substance
If higher concentrations of lipophilic passenger molecules are encapsulated, then the loading capacity increases, but precipitation occurs more rapidly reducing usability
Solution Approach 1:
The patent utilizes parameter changes by adjusting the organic solvent composition (ethanol/isopropanol ratios) and surfactant concentrations to optimize the solubility and stability of lipophilic molecules at high loading concentrations (up to 100-500 mg/mL). This enables maintaining both high quantity of encapsulated substance and long-term stability simultaneously.
Solution Approach 2:
The patent introduces organic solvents (ethanol, isopropanol) and surfactants as intermediary substances that mediate between the lipophilic passenger molecules and the phospholipid vesicle structure. These intermediaries prevent direct precipitation of high concentrations of lipophilic molecules by maintaining their solubility within the vesicle system, enabling high loading without instability.
3Stability of the object's composition
If formulations are prepared at point of use in small batches, then precipitation is avoided initially, but logistical difficulties arise and large-scale use is prevented
Solution Approach 1:
The patent enables preliminary action by formulating stable concentrated stock solutions of lipophilic molecules in organic solvent-based phospholipid vesicles that can be prepared in advance (weeks to months ahead) and stored without precipitation. This eliminates the need for point-of-use preparation while maintaining stability, allowing advance manufacturing and distribution.
Solution Approach 2:
The composite formulation system using organic solvents and surfactants enables stable large-batch preparation by preventing precipitation even at high concentrations during storage. This allows industrial-scale manufacturing of uniform formulations that can be distributed and stored, eliminating logistical constraints of small-batch point-of-use preparation.
4Ease of manufacture
If water is used to close the particles with encapsulated passengers, then the particles can be formed, but lipophilic passengers crystallize and settle to the bottom
Solution Approach 1:
The patent changes the fundamental parameter of the continuous phase from water-based to organic solvent-based (ethanol/isopropanol with surfactants). This parameter change prevents the harmful crystallization and precipitation of lipophilic molecules that occurs in aqueous environments, while still enabling particle formation and stabilization through the phospholipid-surfactant system.
Solution Approach 2:
The patent converts the inherent incompatibility between water and lipophilic molecules (which causes precipitation) into a beneficial organic solvent-based system. By using ethanol or isopropanol as the continuous phase with appropriate surfactants, the formulation naturally accommodates lipophilic molecules, preventing crystallization while maintaining particle stability and enabling high concentrations without the harmful effects seen in aqueous systems.
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 significantly enhances the stability and loading capacity of lipophilic passenger molecules, preventing precipitation and maintaining stability for extended periods, enabling advanced preparation and wider use of formulations, particularly for cannabinoids, with concentrations up to 300 mg/mL achievable.
Implementation Method 1
Disclosed herein is a novel method of encapsulating lipophilic passenger molecules in surfactant-enhanced phospholipid vesicles utilizing one or more surfactants as an encapsulating agent
Data Source
AI summary
A composition comprising surfactant-enhanced phospholipid vesicles with one or more cannabinoid substance encapsulated therein is disclosed, wherein one or more surfactant is utilized for enhancing loading and increasing encapsulation efficiency of cannabinoid passenger molecules within phospholipid structures. A method is disclosed for making a surfactant-enhanced phospholipid vesicles with one or more cannabinoid substance encapsulated therein, wherein one or more surfactant is used for enhancing loading and increasing encapsulation efficiency of passenger molecules in phospholipid structures. A method of using surfactant-enhanced phospholipid vesicles with one or more cannabinoid substance encapsulated therein is disclosed wherein one or more surfactant enhances loading and increases encapsulation efficiency of cannabinoid substances in phospholipid structures. A composition and method of making surfactant-enhanced phospholipid vesicles with one or more lipophilic passenger substance encapsulated therein is disclosed wherein one or more surfactant is utilized for enhancing loading and increasing encapsulation efficiency of passenger molecules within phospholipid structures.