Water-Soluble CBD Composition Using Cyclodextrin Micelles
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Solution Overview
Problem
CBD is poorly soluble in aqueous solutions, limiting its bioavailability and formulation in products like solutions, eye drops, and injections, and there is a need for a new formulation that enhances its solubility and absorption in the human body.
Innovation Solution
Formulating CBD with beta-cyclodextrin and poloxamer to create water-soluble compositions, specifically using a 1:1:0.03 molar ratio, which increases solubility and bioavailability by forming micelles.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If CBD is formulated in lipid-based formulations, then CBD can be delivered, but solubility in aqueous solutions remains poor and bioavailability is limited
Solution Approach 1:
The patent uses cyclodextrins as intermediary molecules that form inclusion complexes with CBD. The cyclodextrin's hydrophilic exterior and hydrophobic interior allow it to solubilize the lipophilic CBD in aqueous environments, acting as a mediator between the poorly soluble CBD and the aqueous formulation medium.
Solution Approach 2:
The invention creates composite formulations combining CBD with cyclodextrins and other excipients. This composite approach allows the formulation to exhibit properties that neither component alone could achieve, specifically achieving both aqueous solubility and maintained CBD activity through the synergistic combination of materials.
2Ease of operation
If CBD is formulated as aqueous solutions for better bioavailability, then absorption is improved, but CBD's inherent poor solubility in water creates formulation challenges
Solution Approach 1:
The patent changes the physical-chemical parameters of the formulation by introducing cyclodextrins that alter the solubility characteristics. This parameter change allows CBD to be formulated in aqueous solutions at concentrations that would otherwise be impossible, transforming the formulation from infeasible to feasible.
Solution Approach 2:
Cyclodextrins serve as intermediary agents that bridge the gap between CBD's lipophilic nature and the hydrophilic formulation requirements. These intermediaries enable the creation of stable aqueous formulations without requiring complex lipid-based delivery systems.
3Ease of manufacture
If lipid-based formulations are used for CBD, then formulation is possible, but the complexity of the formulation process increases
Solution Approach 1:
By using cyclodextrins as intermediary solubilizing agents, the formulation process becomes simpler and more direct. Instead of requiring complex lipid-based delivery systems, the cyclodextrin-mediated approach allows for straightforward aqueous formulation with reduced manufacturing complexity.
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 water-soluble CBD compositions demonstrate enhanced solubility in water, with a solubility of 1.0 g/100 ml at 20°C, and show significant reduction in pro-inflammatory cytokine production, offering therapeutic potential in conditions like COVID-19.
Implementation Method 1
Formulating CBD with beta-cyclodextrin and poloxamer to create water-soluble compositions, specifically using a 1:1:0.03 molar ratio, which increases solubility and bioavailability by forming micelles
Data Source
AI summary
The present invention relates generally to a method of formulation of cannabidiol (CBD) a potential anti-inflammatory drug derived from lemon peel (d-limonene). More, particularly, the present invention relates to the enhancement of lipid soluble CBD into water soluble form in order to improve the formulation of the active component while apply in human for medication. The present invention further provides the therapeutic application of the new formulation which either neutralize and/or decreases the capability of the production of cytokines by activated immune cells during inflammatory process and hence alleviate the sufferings of illness like COVID-19 caused by SARSCOV2.