Gelled Oil-in-Water Emulsion for Cannabinoid Bioavailability
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Solution Overview
Problem
Current delivery methods for cannabinoids, such as oral solid dosage forms and inhalation, face challenges with low bioavailability due to first-pass metabolism and difficulty in controlling the dose, especially for pediatric and elderly patients, and are prone to degradation and irritation.
Innovation Solution
Development of a gelled oil-in-water emulsion that stabilizes cannabinoids, preventing oxidation and coalescence, and enhances oromucosal delivery by forming a self-supporting, viscoelastic solid with micro- or nanoparticles, reducing first-pass metabolism and improving bioavailability.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If oral solid dosage formulations or oral solutions are used for cannabinoid delivery, then administration is simplified, but bioavailability is reduced due to first-pass metabolism
Solution Approach 1:
The patent changes the physical state of the aqueous phase from liquid to gel, creating a semi-solid formulation that maintains oral administrability while enabling oromucosal delivery. This parameter change allows the formulation to be held in the mouth for enhanced absorption through the mucous membranes, bypassing first-pass metabolism and improving bioavailability
Solution Approach 2:
The gelled formulation acts as an intermediary vehicle that enables oromucosal delivery of cannabinoids. The gel structure allows the formulation to be retained in the oral cavity, serving as a mediator between traditional oral administration and sublingual/buccal delivery methods, thereby improving absorption while maintaining ease of administration
2Reliability
If lipid formulations are used to increase cannabinoid absorption, then bioavailability improves, but absorption remains slow with maximum plasma concentrations achieved from 1 to 6 hours after administration
Solution Approach 1:
The patent changes the physical state of the aqueous phase from liquid to gel, creating a semi-solid formulation that melts or dissolves in the oral cavity. This parameter change enables faster release and absorption of cannabinoids through the oromucosal membranes, achieving rapid plasma concentrations similar to sublingual/buccal delivery while maintaining ease of administration
Solution Approach 2:
The gel formulation undergoes phase transition from a semi-solid gel state to a liquid state in the oral cavity, facilitating rapid release and absorption of cannabinoids. This phase transition enables fast absorption through the oromucosal membranes while maintaining the formulation's stability during storage and ease of administration
3Reliability
If sublingual delivery is used to provide faster absorption and reduced first-pass effect, then bioavailability improves, but dose control becomes difficult and convenience is reduced for pediatric and elderly patients
Solution Approach 1:
The patent changes the physical state of the aqueous phase from liquid to gel, creating a semi-solid formulation that can be easily administered to pediatric and elderly patients. The gelled formulation maintains its shape and can be placed in the mouth without spilling, improving ease of administration while enabling oromucosal delivery for rapid absorption and reduced first-pass metabolism
Solution Approach 2:
The gelled formulation creates an equipotential delivery system that combines the advantages of sublingual/buccal delivery (rapid absorption, reduced first-pass effect) with the ease of oral administration. The gel structure allows the formulation to be held in the mouth at the same effectiveness as sublingual delivery, making it equally effective for rapid absorption while being more convenient for various patient populations
4Ease of operation
If cannabinoids are delivered in solution form, then administration is simplified, but degradation occurs due to oxidation and coalescence
Solution Approach 1:
The patent changes the physical state of the aqueous phase from liquid to gel, creating a semi-solid formulation that stabilizes the emulsion. The gelled structure prevents coalescence of oil droplets and reduces oxidation of cannabinoids by limiting molecular mobility and exposure to oxygen, thereby improving formulation stability while maintaining administration simplicity
Solution Approach 2:
The gel network structure provides beforehand cushioning protection against degradation mechanisms. The gel matrix physically separates and stabilizes oil droplets, preventing coalescence before it can occur, and reduces oxidation by limiting contact between cannabinoids and oxygen, thereby protecting the formulation integrity during storage
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 gelled emulsion provides a stable and controlled delivery of cannabinoids with enhanced bioavailability, minimizing first-pass metabolism and improving patient compliance, especially for pediatric and elderly patients, while protecting the active ingredients from degradation.
Implementation Method 1
combining said oil phase and said aqueous phase to form an oil-in-water emulsion
Implementation Method 2
allowing said emulsion to gel
Implementation Method 3
stabilizes cannabinoids, preventing oxidation and coalescence
Implementation Method 4
forming a self-supporting, viscoelastic solid
Data Source
AI summary
The invention relates to compositions for oral administration which contain at least one cannabinoid, to methods for their preparation and to their use as pharmaceuticals or nutraceuticals. In particular, it relates to orally administrable, gelled oil-in-water emulsions which are self-supporting, viscoelastic solids having a gelled aqueous phase and an oil phase which comprises one or more physiologically tolerable lipids and at least one cannabinoid.