Corticosteroid Solubilization in Liquid Oil Esters for Topical Delivery
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Solution Overview
Problem
Topical corticosteroids, especially superpotent and potent ones, cause significant systemic side effects due to high potency, limiting their use duration and effectiveness in chronic skin conditions like psoriasis, as they can lead to hypothalamic-pituitary-adrenal axis suppression and other adverse reactions.
Innovation Solution
A pharmaceutical composition for topical application with a reduced concentration of corticosteroids (less than 0.05% w/w) solubilized in a liquid oil component containing monocarboxylic acid esters and/or dicarboxylic acid esters, which maintains potency and reduces systemic absorption, thereby minimizing side effects.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If superpotent and potent topical corticosteroids are used to treat chronic skin conditions, then dermatological efficacy is improved, but systemic side effects increase
Solution Approach 1:
The patent changes the concentration parameter of corticosteroids from conventional high levels (0.05% or higher) to reduced levels (0.01%-0.04%), and modifies the formulation parameters by incorporating specific liquid oil components (monocarboxylic acid esters and/or dicarboxylic acid esters) to maintain therapeutic efficacy at lower concentrations, thereby reducing systemic absorption and side effects
Solution Approach 2:
The patent creates a composite formulation by combining corticosteroids with specific liquid oil components (monocarboxylic acid esters and/or dicarboxylic acid esters) that enhance drug delivery and maintain potency at reduced concentrations, allowing effective treatment with lower systemic exposure
2Duration of action of stationary object
If high concentration corticosteroids are used, then treatment duration is limited due to side effects, but longer treatment is needed for chronic conditions
Solution Approach 1:
By changing the corticosteroid concentration parameter to reduced levels (0.01%-0.04%) and modifying the formulation composition with specific liquid oil components, the patent enables extended treatment durations for chronic skin conditions without reaching the threshold for systemic side effects that would limit therapy
3Object-affected harmful factors
If corticosteroid concentration is reduced, then systemic absorption decreases, but dermatological potency may be compromised
Solution Approach 1:
The patent formulates a composite material combining corticosteroids with liquid oil components (monocarboxylic acid esters and/or dicarboxylic acid esters) that enhance local drug delivery and maintain dermatological potency at reduced concentrations, ensuring effective treatment while minimizing systemic absorption
Solution Approach 2:
The patent optimizes the concentration parameter of corticosteroids (0.01%-0.04%) and adjusts formulation parameters by incorporating specific liquid oil components to maintain adequate dermatological potency while reducing systemic 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 composition provides sustained dermatological effects with reduced systemic exposure, allowing longer treatment durations for chronic skin conditions without increased systemic side effects, enhancing safety and efficacy.
Implementation Method 1
a liquid oil component comprising one or more monocarboxylic acid esters and/or dicarboxylic acid esters, wherein the liquid oil component further comprises a corticosteroid at a concentration less than 0.05% (w/w), and wherein at least 25% of the corticosteroid is solubilized in the liquid oil component
Data Source
AI summary
Pharmaceutical compositions for topical application to skin are provided. In some embodiments, the pharmaceutical compositions comprise a corticosteroid and further comprise a liquid oil component comprising one or more dicarboxylic acid esters and/or monocarboxylic acid esters.