Topical Corticosteroid Spray with Oleyl Alcohol
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Solution Overview
Problem
Current topical corticosteroid formulations for treating inflammatory skin disorders like psoriasis face challenges such as poor solubility in aqueous vehicles, skin irritation, and inconvenient application methods, leading to suboptimal delivery and increased irritation.
Innovation Solution
An aqueous-based topical spray composition containing betamethasone as the corticosteroid, oleyl alcohol as a skin penetration enhancer, and pharmaceutically acceptable excipients, which is propellant-free and non-foaming, allowing for improved skin penetration and reduced irritation.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If occlusive dosage forms (ointments) are used to improve penetration of corticosteroid into skin layers, then absorption is improved, but greasy sensation and irritation are created
Solution Approach 1:
The patent changes the physical state of the dosage form from occlusive ointment to non-occlusive aerosol spray, and changes the chemical composition by using betamethasone dipropionate in a propellant-based formulation. This allows the drug to be delivered in a non-greasy, evaporating vehicle that reduces skin irritation while maintaining penetration efficiency through the use of penetration enhancers and fine spray droplet delivery.
2Ease of operation
If solution based topical compositions are used, then evaporation occurs before active agent penetrates epidermis, but application convenience is improved
Solution Approach 1:
The patent utilizes phase transition by formulating the corticosteroid as a suspension in a propellant that rapidly evaporates after application. The fine spray droplets transition from liquid to vapor phase, leaving the active agent behind on the skin surface for subsequent penetration, thus preventing premature evaporation loss while maintaining application convenience.
3Ease of operation
If propellant-containing aerosol compositions are used, then application convenience and penetration are improved, but price increases
Solution Approach 1:
The patent uses common propellants (hydrofluoroalkanes) that serve multiple functions: they provide the aerosol spray delivery mechanism for application convenience, act as solvents and co-solvents for the corticosteroid, and facilitate rapid evaporation for efficient drug delivery. This multi-functionality reduces the need for additional expensive excipients.
4Reliability
If alcohol is added to topical compositions, then penetration is improved, but irritation and stinging occur
Solution Approach 1:
The patent changes the chemical composition of the formulation by using betamethasone dipropionate (a more lipophilic ester) instead of betamethasone base, and uses a propellant-based vehicle with specific co-solvents that provide penetration enhancement without the irritant effects of alcohol. The formulation achieves penetration through the combined effect of the ester form and propellant vehicle rather than alcohol.
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 composition achieves effective delivery of the active agent with reduced skin irritation and improved convenience, providing equal or superior efficacy to marketed products while maintaining stability and ease of use.
Implementation Method 1
a fatty alcohol acting as a skin penetration enhancer, wherein the fatty alcohol comprises oleyl alcohol
Implementation Method 2
an aqueous based topical spray composition comprising: a) a corticosteroid which is a betamethasone compound
Implementation Method 3
d) water ; and e) wherein the composition is free of propylene glycol, free of propellant and substantially non-foaming
Data Source
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AI summary
Compositions for the topical administration of an active agent comprising a corticosteroid and a fatty alcohol as skin penetration enhancer, in the form of topical sprays. Processes for preparing such compositions and methods of using them in management of skin diseases or disorders such as psoriasis, dermatoses, and other associated skin diseases or disorders.