Water-Soluble Phytocannabinoid Formulations Using Non-Ionic Surfactants
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Solution Overview
Problem
The limited bioavailability of phytocannabinoids like cannabidiol due to their hydrophobic and insoluble nature in water hinders their therapeutic effectiveness when administered orally, as they are not readily absorbed in the gastrointestinal tract and do not form stable, clear water-soluble solutions.
Innovation Solution
Formulating water-soluble phytocannabinoid formulations by combining phytocannabinoids with non-ionic surfactants, such as polyoxyl castor oil, to create stable, clear solutions that enhance bioavailability, which can be administered in various forms like beverages or liquid concentrates.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If phytocannabinoids are administered orally in traditional formulations, then they can be easily administered, but their bioavailability is limited due to hydrophobicity and water insolubility
Solution Approach 1:
The patent uses non-ionic surfactants as intermediary substances to bridge the gap between hydrophobic phytocannabinoids and aqueous environments. The surfactant molecules have both hydrophobic regions that interact with the phytocannabinoids and hydrophilic regions that interact with water, enabling the formation of stable micellar structures that solubilize the phytocannabinoids while maintaining their bioavailability
Solution Approach 2:
The patent changes the physical-chemical parameters of the phytocannabinoid formulation by adjusting the surfactant concentration, micelle size, and formulation composition. These parameter changes transform the phytocannabinoids from an insoluble state to a solubilized state within micellar structures, thereby improving their aqueous solubility and bioavailability without altering the phytocannabinoid molecule itself
2Reliability
If phytocannabinoids are formulated as water-soluble solutions, then bioavailability is enhanced, but stability and clarity of the solution are compromised due to hydrophobic aggregation
Solution Approach 1:
Non-ionic surfactants serve as mediators that prevent hydrophobic aggregation of phytocannabinoids in aqueous solutions. The surfactants form protective micellar structures around the phytocannabinoid molecules, preventing them from aggregating while maintaining their solubility in water, thus achieving both enhanced bioavailability and solution stability
Solution Approach 2:
The patent creates composite formulations consisting of phytocannabinoids, non-ionic surfactants, and auxiliary ingredients working together. This composite structure combines the hydrophobic phytocannabinoids with the amphiphilic surfactants to form stable micellar complexes that maintain both solubility and stability in aqueous environments
3Reliability
If natural phytocannabinoid compounds are used, then therapeutic properties are maintained, but water solubility is insufficient for convenient formulation delivery
Solution Approach 1:
The non-ionic surfactant acts as an intermediary that enables the delivery of natural phytocannabinoids in water-based formulations. By forming micellar structures, the surfactant allows these hydrophobic therapeutic compounds to be incorporated into convenient liquid formulations such as beverages, syrups, and injectables without compromising their natural therapeutic properties
Solution Approach 2:
The patent creates a universal formulation platform using non-ionic surfactants that can accommodate multiple different phytocannabinoid compounds. This multi-functional approach allows the same surfactant-based delivery system to be used for various phytocannabinoids with different therapeutic indications, enabling convenient formulation delivery across different therapeutic applications
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 use of non-ionic surfactants significantly increases the bioavailability of phytocannabinoids, as demonstrated by enhanced absorption rates in animal studies, achieving higher plasma concentrations and extended duration of action compared to traditional formulations.
Implementation Method 1
combining phytocannabinoids with non-ionic surfactants, such as polyoxyl castor oil, to create stable, clear solutions that enhance bioavailability
Implementation Method 2
The use of non-ionic surfactants significantly increases the bioavailability of phytocannabinoids... achieving higher plasma concentrations
Data Source
AI summary
Methods and formulations for increasing the water solubility and/or bioavailability of a phytocannabinoid compound is disclosed herein. In one example, a water-soluble phytocannabinoid formulation can comprise a phytocannabinoid; a non-ionic surfactant; and optionally, water. The weight ratio of phytocannabinoid content to non-ionic surfactant can be from 1:10,000 to 1:5.