THC Ophthalmic Emulsion Composition for Stable Glaucoma Delivery
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Solution Overview
Problem
Existing ophthalmic drug delivery systems for lipophilic drugs, such as THC, face challenges with formulation stability, solubility, and patient comfort, particularly in aqueous-based eye drops, which affect their efficacy in treating conditions like glaucoma.
Innovation Solution
Development of stable emulsion compositions comprising THC, oil, surfactant, and water, with specific ratios and processing methods to create oil-in-water emulsions that maintain stability and effective drug delivery to the eye, avoiding preservatives and ensuring chemical and microbiological stability.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If lipophilic drugs like THC are formulated in aqueous-based eye drops, then patient comfort and ease of administration are improved, but drug solubility and stability deteriorate
Solution Approach 1:
The patent changes the physical-chemical parameters of the formulation by using emulsion technology to create a system where lipophilic THC can be dispersed in an aqueous base. The emulsion droplets (50-500 nm size) provide a stable interface between the lipophilic drug and aqueous vehicle, maintaining both solubility and patient comfort.
Solution Approach 2:
The patent creates a composite emulsion system combining lipophilic components (THC, oils) with hydrophilic components (aqueous base, surfactants). This composite structure allows the formulation to simultaneously provide patient comfort from the aqueous base while maintaining drug solubility through the lipophilic emulsion droplets.
2Stability of the object's composition
If traditional lipophilic dosage forms (oil solutions, lotions, gels) are used, then drug solubility is improved, but patient comfort and tolerability deteriorate
Solution Approach 1:
The patent transforms the formulation from a traditional lipophilic dosage form to a fine emulsion with controlled droplet size (50-500 nm). This parameter change reduces viscosity and improves spreadability while maintaining drug solubility, thereby enhancing patient comfort without sacrificing solubility.
Solution Approach 2:
The patent segments the lipophilic drug into fine emulsion droplets dispersed in an aqueous continuous phase. This segmentation allows the formulation to maintain drug solubility within the droplets while the aqueous continuous phase provides patient comfort and ease of administration.
3Quantity of substance
If emulsion formulations are developed to improve solubilization, then drug delivery efficacy is improved, but formulation stability and manufacturability deteriorate
Solution Approach 1:
The patent optimizes critical parameters including droplet size (50-500 nm), surfactant concentration, and oil phase composition to achieve both high drug delivery efficacy and formulation stability. These parameter optimizations enable the emulsion to remain stable during manufacturing and storage while effectively delivering the lipophilic drug.
Solution Approach 2:
The patent uses surfactants as intermediary substances that stabilize the interface between lipophilic and hydrophilic phases. These surfactants prevent emulsion breakdown and phase separation, thereby maintaining formulation stability during manufacturing and storage while enabling effective drug delivery.
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 emulsion compositions provide long-lasting intraocular pressure reduction and are well-tolerated, delivering therapeutically effective THC concentrations while maintaining stability over extended storage periods, suitable for treating ophthalmic conditions like glaucoma.
Implementation Method 1
an emulsion composition comprising: tetrahydrocannabinol (THC), or a derivative thereof; an oil; a surfactant; and water
Implementation Method 2
the emulsion comprises an oil phase component comprising a plurality of oil droplets, dispersed with an aqueous phase component, the emulsion remains stable after being stored at a condition selected from the group consisting of: at least two years at about −18° C.; at least three months at about 4° C.; and at least one month at about 23° C. (or room temperature), such that there is an absence of visible phase separation
Data Source
AI summary
The invention provides emulsion compositions comprising at least one cannabinoid compound, and methods for making the same. The emulsion compositions are stable, well tolerated and are capable of delivering therapeutically effective amounts of cannabinoids to target sites, including sites on the surface of and/or within an eye. Also provided are methods of using the compositions to provide ocular neuroprotection and/or to treat ophthalmic conditions such as glaucoma.