Topical Erlotinib Composition for Pediatric Keratoderma

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Solution Overview

Problem

Current treatments for palmoplantar keratodermas, such as Olmsted syndrome and pachyonychia congenita, often result in severe side effects when erlotinib is administered systemically, making it unsuitable for children, and existing topical treatments are inadequate for effectively managing these conditions.

Innovation Solution

A topical composition comprising erlotinib, in concentrations ranging from 0.01 to 10% combined with pharmaceutically acceptable excipients, including penetration enhancers like ethanol and cyclodextrin, is applied directly to the skin of children under 15 years old, specifically targeting palmoplantar keratoderma conditions like Olmsted syndrome and pachyonychia congenita.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If erlotinib is administered systemically to treat keratodermas, then therapeutic activity is achieved, but severe side effects occur making it unsuitable for children

Engineering Contradiction:
Improvetherapeutic activityVSAvoidsystemic side effects
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The treatment approach is segmented by switching from systemic administration to localized topical application. The erlotinib is delivered as a topical composition applied directly to affected skin areas, segmenting the therapeutic action from the whole body to specific keratoderma lesions, thereby achieving local therapeutic efficacy while avoiding systemic side effects in children

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The patent applies local quality by creating a topical composition with specific formulation characteristics (including penetration enhancers and appropriate concentrations of erlotinib) that enables the drug to act locally on keratoderma lesions. This localized delivery ensures the medication works where needed without exposing the entire body to systemic effects

Inventive Principle:
Principle #3Local quality

2Object-affected harmful factors

If existing topical treatments are used for keratodermas, then local application is avoided, but they are inadequate for effectively managing these conditions

Engineering Contradiction:
Improvesystemic side effectsVSAvoidtherapeutic efficacy
Core Design Contradiction:
Object-affected harmful factorsVSReliability

Solution Approach 1:

The patent achieves effective topical treatment by optimizing key parameters of the erlotinib composition including concentration (0.01-10% w/w), pH (4-8), and incorporating penetration enhancers at specific concentrations. These parameter adjustments ensure sufficient drug penetration through the hyperkeratotic skin while maintaining safety and efficacy for pediatric patients

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The topical composition is formulated as a composite material combining erlotinib with pharmaceutically acceptable excipients, penetration enhancers (such as ethanol, cyclodextrin, or fatty acids), and emollients. This composite formulation enhances drug delivery through thickened skin while maintaining patient comfort and safety

Inventive Principle:
Principle #40Composite materials

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 topical administration of erlotinib minimizes systemic side effects while providing therapeutic activity, effectively treating keratoderma conditions by delivering erlotinib directly to the affected skin areas, thereby reducing pain and hyperkeratosis in children.

Implementation Method 1

a pharmaceutically acceptable excipient, preferably the composition comprises a penetration enhancer

Methodology Applied
Scientific EffectPenetration enhancement: Permeation

Data Source

PatentUS20230149405A1Topical use of erlotinib for treating keratodermas in children
Publication Date: 2023.05.18 LAB CTRS
  • US20230149405A1 patent drawing

AI summary

A topical composition including erlotinib and a pharmaceutically acceptable excipient for use in the treatment of a keratoderma in a child, preferably a palmoplantar keratoderma (PPK), wherein the composition is topically administered. The composition may further include a penetration enhancer. The treated subject may be younger than three years old. Also, woven or non-woven fabric support including erlotinib and to dressings, patches, gloves and socks having the support useful in the treatment of a PPK.