Cannabinoid Solubilization via Phospholipid Micelles
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Solution Overview
Problem
Existing methods for solubilizing cannabinoids face challenges due to the highly lipophilic nature of these compounds, leading to poor bioavailability and variability in oral dosage forms, which are exacerbated by the use of potentially harmful emulsifiers like polysorbates and polyethylene glycols, making them unsuitable for long-term use.
Innovation Solution
A solubilization method using medium-chain triglycerides, non-hydrogenated phosphatidylcholine, non-hydrogenated lysophosphatidylcholine, C2-C4 alcohols, and saturated or unsaturated C14-C20 fatty acids, combined with ultrasonic treatment, to create a solubilisate without polysorbates or polyethylene glycols, ensuring stable and effective solubilization of cannabinoids.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Quantity of substance
If traditional emulsifiers like polysorbates and polyethylene glycols are used to solubilize cannabinoids, then solubility is improved, but safety and suitability for long-term use deteriorate
Solution Approach 1:
The patent changes the chemical parameters of the solubilization system by replacing synthetic emulsifiers (polysorbates, polyethylene glycols) with natural phospholipids (lecithin) and medium-chain triglycerides. This parameter change maintains solubilization effectiveness while eliminating the harmful effects associated with traditional emulsifiers, making the formulation safe for long-term use.
Solution Approach 2:
The patent employs a composite solubilization system consisting of phospholipids (lecithin), medium-chain triglycerides, and C2-C4 alcohols. This composite approach combines multiple natural substances that work synergistically to solubilize lipophilic cannabinoids, achieving both solubility enhancement and safety requirements without relying on harmful synthetic emulsifiers.
2Manufacturing precision
If oral dosage forms are developed for cannabinoids, then controlled dosing is improved, but bioavailability deteriorates due to poor water solubility
Solution Approach 1:
The patent introduces phospholipids and medium-chain triglycerides as intermediary substances that mediate between the lipophilic cannabinoids and the aqueous environment. These intermediaries form micellar structures that encapsulate cannabinoids, enabling them to be transported through the gastrointestinal tract and absorbed into the bloodstream, thus improving bioavailability while maintaining controlled dosing.
Solution Approach 2:
The patent changes the physical-chemical parameters of the cannabinoid formulation by converting it from a pure lipophilic substance to a micellar complex with improved hydrophilicity. This parameter change enables the cannabinoid to dissolve in aqueous media, cross intestinal membranes, and achieve reliable bioavailability while preserving precise dosing control.
3Reliability
If micelle and liposome technologies are used to improve solubility, then bioavailability is improved, but device complexity and production costs increase
Solution Approach 1:
The patent employs a self-assembling micellar system where phospholipids and medium-chain triglycerides automatically form micelles upon contact with water, encapsulating cannabinoids in the process. This self-service mechanism eliminates the need for complex external equipment or multi-step processing, achieving improved bioavailability through a simple, scalable formulation approach.
Solution Approach 2:
The patent uses inexpensive, readily available natural substances (lecithin, medium-chain triglycerides) to create a simple micellar formulation. This approach replaces complex, expensive liposome technologies with a more economical micellar system that achieves comparable bioavailability improvement through a simpler, more cost-effective formulation.
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 method achieves nearly complete solubilization of cannabinoids, allowing for improved bioavailability and stability, without the adverse effects associated with traditional emulsifiers, suitable for both pharmaceutical and dietary supplement applications.
Implementation Method 1
the use of ultrasonic treatment in a frequency range of 20 kHz to 1 MHz and a power range of 50 W to 40 KW
Implementation Method 2
Heating the mixture of step c) by continuously increasing the temperature with a temperature increment of 0.5°C/min to 5°C/min until a final temperature of 100°C to 130°C is reached
Implementation Method 3
A third solubilization mechanism are micelle and liposome application technologies. They have won broad attention throughout the last decades. Herein the substance to be delivered is enclosed in a spherical aggregate of surfactant molecules
Implementation Method 4
Herein the solubility of an agent in a medium is augmented by adding a third substance. These third substances are referred to as solubilizers (solubilizing agents), substances that may for example build a complex with the substance to be solubilized
Data Source
AI summary
The present invention relates to a method for solubilizing phytogenic, endogenous and synthetic cannabinoids, to the solubilisate produced by this method and respective uses as a pharmaceutical dosage form. A MCT oil- and non-hydrogenated phosphatidylcholine-based solubilization method is disclosed.