Donepezil Nanofiber Transdermal Patch for Alzheimer's

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Solution Overview

Problem

Current oral donepezil formulations for Alzheimer's disease treatment are associated with significant side effects and inadequate dosage control, and existing transdermal forms fail to provide consistent drug release.

Innovation Solution

Development of donepezil-containing nanofibers using the electrospinning method, which creates a transdermal drug delivery system in patch or plaster form with a controlled release mechanism, utilizing biocompatible polymers and surfactants to ensure optimal homogeneity and controlled drug release.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of operation

If oral donepezil formulations are used, then the drug can be administered conveniently, but significant side effects occur including nausea, diarrhea, insomnia, vomiting, and gastrointestinal ailments

Engineering Contradiction:
Improveconvenience of administrationVSAvoidside effects
Core Design Contradiction:
Ease of operationVSObject-generated harmful factors

Solution Approach 1:

The patent introduces a transdermal delivery system as an intermediary between the drug and the body's internal systems. The donepezil is delivered through the skin rather than being ingested, using a patch or plaster that releases the drug through the skin barrier into the bloodstream, thereby avoiding direct contact with the gastrointestinal tract and reducing GI side effects

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent replaces the mechanical/oral ingestion route with a transdermal delivery mechanism. Instead of swallowing tablets or capsules that travel through the digestive system, the drug is delivered through electrospun nanofibers that release donepezil through the skin, substituting the oral-mechanical pathway with a transdermal-physiological pathway

Inventive Principle:
Principle #28Mechanics substitution (Replace mechanical system)

2Object-generated harmful factors

If delayed release oral formulations are used, then side effects are alleviated to some extent, but they are not eliminated entirely and patient compliance remains insufficient

Engineering Contradiction:
Improveside effectsVSAvoidpatient compliance
Core Design Contradiction:
Object-generated harmful factorsVSReliability

Solution Approach 1:

The patent changes the delivery parameter from oral delayed-release to transdermal controlled-release. The electrospun nanofiber matrix provides sustained release of donepezil through the skin, maintaining steady drug levels in the bloodstream over extended periods (up to 7 days), which eliminates the need for frequent dosing and significantly improves patient compliance while fully eliminating GI side effects

Inventive Principle:
Principle #35Parameter changes

3Object-generated harmful factors

If conventional transdermal applications are used, then side effects are reduced, but the drug dosage cannot be controlled properly and necessary dosage cannot be provided in desired periods

Engineering Contradiction:
Improveside effectsVSAvoiddosage control
Core Design Contradiction:
Object-generated harmful factorsVSManufacturing precision

Solution Approach 1:

The patent utilizes electrospun nanofibers with controlled porosity to achieve precise dosage control. The porous structure of the nanofiber mat allows for controlled diffusion of donepezil at predetermined rates, enabling accurate dosing over extended periods while maintaining the benefits of transdermal delivery and avoiding the dosage control problems of conventional transdermal patches

Inventive Principle:
Principle #31Porous materials

4Object-generated harmful factors

If oral formulations are used, then high gastric acid secretion occurs due to cholinergic activity, but changing to transdermal forms previously failed to provide consistent release

Engineering Contradiction:
Improvegastric acid secretionVSAvoiddrug release consistency
Core Design Contradiction:
Object-generated harmful factorsVSStability of the object's composition

Solution Approach 1:

The patent employs composite electrospun nanofiber materials comprising biocompatible polymers (such as poly(lactic-co-glycolic acid) or polyethylene glycol) blended with donepezil. This composite structure provides both the controlled release properties needed for consistent drug delivery and the transdermal delivery mechanism needed to eliminate gastric acid secretion issues, achieving both goals simultaneously

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 nanofiber-based transdermal system provides a consistent and prolonged release of donepezil, reducing side effects and improving patient compliance, with enhanced bioavailability and stability of the active ingredient.

Implementation Method 1

electrospinning method is specifically preferred for obtaining nanofibers. This method is advantageous in obtaining broadened surface area and increased porousness transdermal dosage forms

Methodology Applied
Scientific EffectElectrospinning: Electrohydrodynamics

Data Source

PatentEP2810645B1New Drug Delivery System
Publication Date: 2017.05.24 GENCTURK ASLI
  • EP2810645B1 patent drawingFigure 1
  • EP2810645B1 patent drawingFigure 2~3
  • EP2810645B1 patent drawingFigure 4

AI summary

The present invention relates to the use of nanofibers comprising donepezil or a pharmaceutically acceptable salt thereof as active ingredient and at least one polymer as a transdermal dosage form for treatment of Alzheimer type dementia.