Crisaborole Topical Formulation for Stable, Low-Irritation Eczema Care

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Solution Overview

Problem

Existing topical formulations for skin conditions lack optimal balance between occlusivity and breathability, stability, and safety, while also requiring pleasant texture, easy spreadability, and hypoallergenic properties to enhance patient adherence and treatment outcomes.

Innovation Solution

A topical composition comprising a PDE4 inhibitor, solubilizer, humectant, preservatives, and buffering agents, with specific concentrations of crisaborole, ethanol, propylene glycol, lauramine oxide, sodium citrate, and citric acid, maintains stability and efficacy for treating eczema, while using an applicator for easy application.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Stability of the object's composition

If the formulation increases occlusivity to improve moisture retention, then moisture retention is improved, but breathability deteriorates and may exacerbate skin conditions

Engineering Contradiction:

Improvemoisture retentionVSAvoidexcessive occlusion

Core Design Contradiction:

Stability of the object's compositionVSObject-affected harmful factors

Solution Approach 1:

The formulation adjusts the concentration and type of occlusive agents to achieve optimal moisture retention while preventing excessive occlusion. By carefully controlling the parameters of occlusivity, the formulation maintains therapeutic benefits without causing adverse effects from over-occlusion.

Inventive Principle:

Principle #35Parameter changes

2Reliability

If the formulation includes multiple active ingredients to improve therapeutic effectiveness, then therapeutic benefits are improved, but formulation stability and safety deteriorate

Engineering Contradiction:

Improvetherapeutic effectivenessVSAvoidformulation stability

Core Design Contradiction:

ReliabilityVSStability of the object's composition

Solution Approach 1:

The formulation combines multiple active ingredients (PDE4 inhibitor, solubilizer, humectant, preservatives, buffering agents) into a composite topical composition. Each ingredient serves a specific function while being compatible with others, achieving synergistic therapeutic effects while maintaining overall formulation stability through careful selection and concentration control.

Inventive Principle:

Principle #40Composite materials

3Reliability

If the formulation uses common irritants and allergens to enhance therapeutic effect, then therapeutic benefits are improved, but hypoallergenic properties deteriorate and risk of sensitization increases

Engineering Contradiction:

Improvetherapeutic effectVSAvoidsensitization risk

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The formulation extracts and eliminates common irritants and allergens (such as fragrances) from the composition while retaining essential therapeutic ingredients. This selective removal approach maintains therapeutic effectiveness for eczema treatment while significantly reducing the risk of sensitization and adverse reactions.

Inventive Principle:

Principle #2Taking out (Extraction)

4Ease of operation

If the formulation has quick absorption to improve patient adherence, then ease of operation is improved, but occlusivity and moisture retention deteriorate

Engineering Contradiction:

Improveabsorption speedVSAvoidmoisture retention

Core Design Contradiction:

Ease of operationVSStability of the object's composition

Solution Approach 1:

The formulation achieves dynamic performance by providing quick initial absorption for patient comfort and adherence, while simultaneously maintaining sufficient occlusivity for ongoing moisture retention. The composition balances fast penetration with sustained protective film formation on the skin surface.

Inventive Principle:

Principle #15Dynamics

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 formulation provides stable, effective, and easy-to-apply treatment for eczema with minimal irritation, ensuring therapeutic benefits and patient satisfaction.

Implementation Method 1

The solubilizer is selected from the group consisting of isopropanol and ethanol and is present in a concentration range of 1.0-25.0% w/w

Methodology Applied

Scientific EffectSolubilization: Solvation

Implementation Method 2

Humectants are chosen from the group consisting of propylene glycol and glycerin and are at a concentration of 0.5-10.0% w/w

Methodology Applied

Scientific EffectHumectant action: Absorption (physical)

Implementation Method 3

preservatives such as lauramine oxide, 1,2-hexanediol, and 1,2-octanediol are present in the composition, with each in the range of 0.01-2.0% w/w

Methodology Applied

Scientific EffectPreservation: Preservative

Implementation Method 4

Buffering agents comprise sodium citrate, citric acid, sodium acetate, acetic acid, sodium phosphate monobasic, and sodium phosphate dibasic at concentrations ranging from 0.05-5.0% w/w, and the overall pH of the composition is maintained within a range of 4.5-7.5

Methodology Applied

Scientific EffectBuffering:

Data Source

PatentUS20250275992A1Topical formulations for therapeutically active agents

Publication Date: 2025.09.04 OCUSOFT INC

AI summary

The present invention illustrates formulations designed to deliver active ingredients effectively to the surface of the skin. The formulations comprise therapeutically effective amounts of antihistamine, anti-inflammatory, anesthetic, antioxidant, and anti-eczema active agents. Additional ingredients are included to enhance delivery, stability, and physiological compatibility with the skin. The topical formulations are further configured to be delivered via an applicator to the skin.