Polyaphron Dispersion for Vitamin D Topical Delivery

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Solution Overview

Problem

Current topical compositions containing high concentrations of vitamin D or vitamin D analogues for treating psoriasis often cause skin irritation and worsening of the condition, with issues like hypercalcaemia and high surfactant levels leading to adverse effects.

Innovation Solution

A topical composition comprising a polyaphron dispersion with a continuous and discontinuous phase, using low levels of vitamin D or vitamin D analogues, and minimal surfactants, which enhances dermal diffusion and stability, reducing skin irritation and antropogenic potential, and maintaining stability at elevated temperatures.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If high concentrations of vitamin D or vitamin D analogues are used in topical compositions, then treatment efficacy for psoriasis is improved, but skin irritation and worsening of psoriasis occur

Engineering Contradiction:
Improvetreatment efficacyVSAvoidskin irritation
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent changes the physical-chemical parameters of the vitamin D composition by incorporating it into a polyaphron dispersion system with specific phase ratios and surfactant concentrations, enabling lower effective concentrations to achieve the same therapeutic effect with reduced irritation

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent creates a composite delivery system using polyaphron dispersion comprising continuous and discontinuous phases with surfactants, combining multiple components to achieve controlled release and reduced skin irritation while maintaining treatment efficacy

Inventive Principle:
Principle #40Composite materials

2Productivity

If high levels of surfactants are used in topical compositions, then vitamin D delivery is improved, but hypercalcaemia and adverse effects occur

Engineering Contradiction:
Improvedrug deliveryVSAvoidhypercalcaemia
Core Design Contradiction:
ProductivityVSObject-generated harmful factors

Solution Approach 1:

The patent optimizes the surfactant concentration parameter within a specific range (0.1-10% w/w) in the polyaphron dispersion system, achieving effective drug delivery while minimizing the risk of hypercalcaemia and other adverse effects associated with excessive surfactant use

Inventive Principle:
Principle #35Parameter changes

3Ease of operation

If conventional emulsion formulations are used, then vitamin D can be delivered topically, but the compositions lack stability at elevated temperatures

Engineering Contradiction:
Improvetopical applicationVSAvoidtemperature stability
Core Design Contradiction:
Ease of operationVSStability of the object's composition

Solution Approach 1:

The patent develops a composite polyaphron dispersion formulation with specific phase compositions and ratios that provides enhanced thermal stability compared to conventional emulsions, maintaining structural integrity and drug efficacy at elevated temperatures during storage and application

Inventive Principle:
Principle #40Composite materials

4Reliability

If conventional topical compositions are used, then vitamin D treatment can be applied, but patient compliance is reduced due to skin irritation

Engineering Contradiction:
Improvetreatment effectivenessVSAvoidpatient compliance
Core Design Contradiction:
ReliabilityVSEase of operation

Solution Approach 1:

The patent modifies the formulation parameters by using polyaphron dispersion with controlled phase ratios and optimized surfactant levels, reducing skin irritation and improving patient comfort and compliance while maintaining effective psoriasis treatment

Inventive Principle:
Principle #35Parameter changes

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 drug delivery with reduced skin irritation, improved stability, and lower surfactant concentrations, making it suitable for effective psoriasis treatment with enhanced patient compliance and reduced risk of adverse effects.

Implementation Method 1

The present inventors have surprisingly found that such compositions have an enhanced dermal diffusion rate

Methodology Applied
Scientific EffectDermal diffusion: Diffusion

Implementation Method 2

The compositions also have an agreeable skin feel during and after topical application (which helps to ensure good patient compliance with the treatment regime)

Methodology Applied
Scientific EffectThermal stability:

Data Source

PatentEP2139453B1Polyaphron topical composition with vitamin d
Publication Date: 2011.05.04 DRUG DELIVERYSOLUTIONS LTD
  • EP2139453B1 patent drawingFigure 1~2

AI summary

A topical composition comprising a continuous phase and at least one discontinuous phase, said composition comprising at least one polyaphron dispersion and at least one vitamin D or vitamin D analogue.