Encapsulated Cannabinoid Gels and Patches for Transdermal Bioavailability
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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 high lipophilicity and poor water solubility, limiting their effectiveness in transdermal delivery systems.
Innovation Solution
Development of surfactant-stabilized, water-soluble cannabinoid formulations using optimized hydrophilic-lipophilic balance (HLB) to create self-emulsifying drug delivery systems (SEDDS) that encapsulate cannabinoids in micelles, enhancing stability and bioavailability.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If cannabinoids are formulated with traditional drug delivery methods, then they can be delivered to subjects, but their poor water solubility and high lipophilicity result in low bioavailability
Solution Approach 1:
The patent uses surfactants as intermediary substances to bridge the incompatibility between lipophilic cannabinoids and aqueous delivery systems. The surfactants form micelles with hydrophobic cores that encapsulate cannabinoids, while the hydrophilic outer surfaces enable water solubility and stability in aqueous formulations, thereby improving bioavailability without sacrificing solubility
Solution Approach 2:
The patent changes the physical-chemical parameters of cannabinoid formulations by adjusting the hydrophilic-lipophilic balance (HLB) of surfactant systems. By selecting surfactants with optimal HLB values and combining them in specific ratios, the formulation transforms cannabinoids from insoluble crystalline substances into soluble micellar complexes, enabling effective transdermal and other traditional drug delivery methods
2Reliability
If cannabinoids are made water-soluble through formulation, then bioavailability increases, but formulation complexity increases due to need for surfactants and emulsification systems
Solution Approach 1:
The patent creates composite micellar formulations by combining surfactants with complementary properties. Specifically, it uses a blend of ionic and nonionic surfactants where the ionic surfactant provides strong emulsification and the nonionic surfactant provides steric stabilization. This composite approach achieves superior bioavailability while managing formulation complexity through synergistic interactions between components
3Stability of the object's composition
If micelles are used to encapsulate cannabinoids, then stability and bioavailability increase, but the formulation requires optimized HLB and surfactant blends increasing manufacturing complexity
Solution Approach 1:
The patent performs preliminary optimization of surfactant blends before final formulation manufacturing. By pre-determining the optimal HLB values and surfactant ratio combinations through laboratory studies, the patent establishes standardized formulations that can be manufactured consistently. This preliminary characterization of micellar systems simplifies subsequent manufacturing processes while maintaining high stability and bioavailability
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 through the use of micelles and sustained therapeutic doses over 72 hours.
Implementation Method 1
Above the critical micelle concentration of one or more surfactants that micelles will be formed during emulsification
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 micelles can also be used to encapsulate active ingredients for delivery of pharmaceuticals
Implementation Method 4
Transdermal delivery allows for direct absorption into the bloodstream without a hepatic first pass effect
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), cannabigero (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.