Micellar Cannabinoid Formulations for Sustained Transdermal Delivery
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Solution Overview
Problem
Existing cannabinoid formulations face challenges in achieving increased bioavailability and are not conducive to traditional drug delivery methods due to their poor water solubility and lipophilicity, limiting their effectiveness in transdermal delivery systems.
Innovation Solution
Development of surfactant-stabilized, water-soluble cannabinoid formulations that form micelles with optimized hydrophilic-lipophilic balance (HLB) to create self-emulsifying drug delivery systems (SEDDS) for enhanced encapsulation and stability, allowing for transdermal delivery through oil-in-water emulsions.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If traditional drug delivery methods are used for cannabinoids, then the delivery system is simple and well-established, but the bioavailability is reduced due to poor water solubility and lipophilicity of cannabinoids
Solution Approach 1:
The patent uses micelles as intermediary structures to bridge the hydrophobic cannabinoids and hydrophilic delivery systems. The micelle core encapsulates the lipophilic cannabinoid molecules while the hydrophilic outer shell enables water-based transport and transdermal delivery, resolving the contradiction between cannabinoid lipophilicity and delivery system requirements
Solution Approach 2:
The patent modifies the physical-chemical parameters of cannabinoid delivery by changing from pure oil-based formulations to water-soluble micellar formulations. This parameter change enables the cannabinoids to be transported in aqueous environments, improving bioavailability while maintaining formulation stability
2Reliability
If cannabinoids are made water-soluble through formulation, then bioavailability increases, but the formulation stability may be compromised
Solution Approach 1:
Micelles serve as stable intermediary carriers that prevent cannabinoid aggregation and precipitation in aqueous solutions. The amphiphilic structure of micelles provides both hydrophobic interaction with cannabinoids and hydrophilic interaction with water, maintaining formulation stability while enabling water-solubility
Solution Approach 2:
The patent creates composite micellar formulations combining multiple components (surfactants, co-solvents, cannabinoids) that work synergistically. This composite approach enhances both stability and bioavailability by leveraging the complementary properties of different formulation components
3Reliability
If micelles are used to encapsulate cannabinoids, then water solubility and bioavailability improve, but the formulation complexity increases
Solution Approach 1:
The patent employs self-emulsifying drug delivery systems that automatically form micelles upon contact with water, eliminating the need for complex emulsification equipment. The formulation self-assembles into micelles, reducing manufacturing complexity while maintaining encapsulation efficiency
Solution Approach 2:
The patent optimizes formulation parameters such as HLB values, surfactant concentrations, and co-solvent ratios to achieve stable micelle formation with minimal complexity. By carefully controlling these parameters, the formulation achieves high bioavailability without requiring overly complex preparation procedures
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 formulations achieve increased bioavailability and stability of cannabinoids, enabling effective transdermal delivery with sustained therapeutic effects over 72 hours, reducing skin irritation and enhancing permeation.
Implementation Method 1
Above the critical micelle concentration of one or more surfactants that micelles will be formed during emulsification. The micelles can take many shapes (spherical, cylinders, or other arrangements), structures (unilamellar or multilamellar), and names (liposomes, niosomes, and ethosomes among others).
Implementation Method 2
A blend of surfactants can increase the stability of emulsions and create self-emulsifying drug delivery systems (SEDDS).
Implementation Method 3
The encapsulation protects labile ingredients and the hydrophilic heads of the micellular outer shell increase drug delivery capabilities.
Implementation Method 4
Transdermal delivery allows for direct absorption into the bloodstream without a hepatic first pass effect that significantly reduces the bioavailability of cannabinoids.
Data Source
AI summary
Preparation of cannabinoid formulations containing: Δ9-tetrahydrocannabinol (Δ9-THC), Δ8-tetrahydrocannabinol (Δ8-THC), Δ9-tetrahydrocannabinolic acid (THCa), cannabidiol (CBD), cannabidiolic acid (CBDa), cannabigerol (CBG), cannabichromene (CBC) and cannabinol (CBN), either alone or in combinations henceforth known as cannabis, have been created using an emulsification process to encapsulate cannabinoids. The aqueous-based method involves micellular encapsulation of cannabinoids, a method that has been used to increase the bioavailability of poorly permeable, lipophilic drugs. The present invention demonstrates the viability of transdermal delivery with gels and patches for consistent and sustained cannabinoid dosing.