Polyaphron Dispersion for Topical Vitamin D and Corticosteroid Delivery
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Solution Overview
Problem
Current topical compositions containing vitamin D or vitamin D analogues and corticosteroids for treating psoriasis face issues such as skin irritation, poor skin penetration, and stability challenges due to differing pH requirements, leading to ineffective treatment and patient compliance issues.
Innovation Solution
A composition comprising a polyaphron dispersion with a continuous and discontinuous phase, incorporating vitamin D or vitamin D analogues and corticosteroids, which enhances dermal diffusion and stability, allowing for lower active agent concentrations and improved skin permeation without the need for high surfactant levels or elevated temperatures.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Speed
If high concentrations of vitamin D or vitamin D analogues and surfactants are used to improve skin penetration, then dermal diffusion is enhanced, but skin irritation and worsening of psoriasis occur
Solution Approach 1:
The invention changes the physical state and concentration parameters of the formulation by using a polyaphron dispersion system with low surfactant levels (1-10% w/w) compared to conventional emulsions. This allows achieving effective drug delivery at lower vitamin D concentrations (0.001-0.05% w/w), thereby reducing skin irritation while maintaining therapeutic efficacy.
Solution Approach 2:
The invention uses a composite polyaphron dispersion system combining hydrophilic and hydrophobic phases with specific surfactants to create a unique delivery vehicle. This composite structure enables improved skin penetration without requiring high concentrations of individual components, thus avoiding the skin irritation associated with conventional high-surfactant emulsions.
2Stability of the object's composition
If vitamin D or vitamin D analogues are formulated in wax-based compositions to improve stability, then compound stability is maintained, but the compositions leave a greasy film on skin and require heating to 70°C for manufacturing
Solution Approach 1:
The invention changes the manufacturing temperature parameter from 70°C (wax-based) to room temperature (20-25°C) by using a polyaphron dispersion system. This eliminates the need for heating, preserving drug stability while improving patient compliance through a non-greasy, easily applied formulation.
Solution Approach 2:
The invention extracts the wax component from the formulation, replacing it with a polyaphron dispersion system. This removal of wax eliminates the greasy film problem while maintaining compound stability, and simplifies manufacturing by eliminating the heating step.
3Quantity of substance
If high levels of vitamin D or vitamin D analogue are used in wax-based compositions to achieve beneficial treatment results, then sufficient drug permeation is obtained, but skin irritation increases
Solution Approach 1:
The invention changes the vitamin D concentration parameter from high levels (0.01-0.1% in wax-based) to low levels (0.001-0.05% w/w) in the polyaphron dispersion system. The unique polyaphron structure enhances drug delivery efficiency, allowing effective treatment at lower concentrations and thereby reducing skin irritation.
4Ease of operation
If vitamin D analogue and corticosteroid are combined in a single formulation to simplify treatment, then patient compliance improves, but stability challenges arise due to differing pH requirements
Solution Approach 1:
The invention changes the pH parameter to a neutral range (pH 6-8) that is compatible with both vitamin D analogues and corticosteroids. The polyaphron dispersion system buffers the pH effectively, allowing stable co-formulation of both drugs at their optimal stability conditions, thereby simplifying treatment and improving patient compliance.
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 enhanced skin permeation and stability, reducing skin irritation and improving patient compliance by maintaining effective treatment with lower active agent concentrations and a more pleasant application experience.
Implementation Method 1
enhances dermal diffusion and stability, allowing for lower active agent concentrations and improved skin permeation
Data Source
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Figure 3
AI summary
A composition suitable for topical application comprising a continuous phase and at least one discontinuous phase, said composition comprising at least one polyaphron dispersion, at least one vitamin D or vitamin D analogue and at least one corticosteroid.