PEG Polymer Hydrating Layer for Vaginal Mucosa

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Solution Overview

Problem

Current treatments for vaginal atrophy, such as hormone replacement therapy and plant-based substances, have systemic side effects due to non-local action, and existing polymers for barrier protection may not effectively address the specific hydration needs of the vaginal mucosa.

Innovation Solution

Pharmaceutical compositions in solid form using PEGs with a molecular weight of 3000 or more, combined with surfactants, acidifiers, and disintegrating agents, to create a localized hydrating effect that improves vaginal mucosa trophism without systemic side effects.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If hormone replacement therapy or plant-based substances are used to treat vaginal atrophy, then the therapeutic effect on vaginal mucosa is improved, but systemic side effects occur due to non-local action

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

Solution Approach 1:

The patent applies local quality by using a polymer composition that acts exclusively at the local vaginal level. The polymer matrix with controlled porosity (2-20 micrometers) enables localized drug delivery to the vaginal mucosa, ensuring the therapeutic agent acts only where needed without systemic distribution. This resolves the contradiction by maintaining therapeutic efficacy while eliminating systemic side effects through spatially restricted action.

Inventive Principle:
Principle #3Local quality

Solution Approach 2:

The patent uses a polymer intermediary (crosslinked polyacrylic acid or polyvinyl alcohol) as a delivery vehicle. This polymer matrix absorbs water to form a gel that locally releases the therapeutic agent at the vaginal site. The polymer acts as an intermediary carrier that transports the active ingredient locally without allowing systemic absorption, thus achieving therapeutic effect while avoiding systemic side effects.

Inventive Principle:
Principle #24Intermediary (Mediator)

2Object-affected harmful factors

If barrier polymers are used to protect vaginal mucosa, then protection against pathogenic micro-organisms is improved, but the specific hydration needs of vaginal mucosa are not effectively addressed

Engineering Contradiction:
Improveprotection against pathogenic micro-organismsVSAvoidhydration effect
Core Design Contradiction:
Object-affected harmful factorsVSReliability

Solution Approach 1:

The patent merges two functions into a single polymer composition: (1) barrier protection against pathogenic micro-organisms through the polymer matrix structure, and (2) hydration of vaginal mucosa through water-absorbing capability of the polymer. The crosslinked polymer network simultaneously provides mechanical barrier function and osmotic hydration, resolving the contradiction by combining protective and hydrating functions in one system.

Inventive Principle:
Principle #5Merging (Combining)

Solution Approach 2:

The patent uses composite materials by combining water-absorbing polymers (polyacrylic acid or polyvinyl alcohol) with therapeutic agents and forming a crosslinked gel matrix. This composite structure integrates the barrier properties of the polymer network with the hydrating capability of the hydrophilic polymer chains, achieving both protection and hydration simultaneously.

Inventive Principle:
Principle #40Composite materials

3Reliability

If polymers with high water absorption are used, then hydration of vaginal mucosa is improved, but barrier protection function is reduced

Engineering Contradiction:
Improvehydration effectVSAvoidbarrier protection
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent applies parameter changes by controlling the porosity of the polymer matrix within a specific range (2-20 micrometers) and adjusting the crosslinking degree of the polymer. These parameter optimizations enable the polymer to simultaneously achieve high water absorption for hydration while maintaining sufficient structural integrity for barrier protection. The specific porosity range allows water penetration for hydration while preventing pathogenic micro-organism invasion.

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 compositions provide a stable improvement in vaginal mucosa trophism by forming a hydrating layer, maintaining optimal pH, and inhibiting pathogenic microbes, as demonstrated by significant increases in vaginal secretions and pH levels in clinical trials.

Implementation Method 1

They exert a considerable osmotic attraction on water... the observed effect on trophism takes place unexpectedly, depending on the physical properties... their use would cause water attraction useful for normal basal activities of the target site

Methodology Applied
Scientific EffectOsmotic pressure: Osmotic Pressure

Implementation Method 2

surfactants can be added, i.e. substances that reduce the surface tension of the aqueous medium on the surfaces with which they come into contact, facilitating and standardising the wetting of said surfaces and therefore accelerating the penetration of the water required for hydration

Methodology Applied
Scientific EffectSurfactant: Surfactant

Data Source

PatentEP3501507B1Macrogols for application to the mucosa, and therapeutic uses thereof
Publication Date: 2020.07.15 S I I T SRL
  • EP3501507B1 patent drawingFigure 1
  • EP3501507B1 patent drawingFigure 2

AI summary

The present invention relates to the use of pharmaceutical compositions in solid form containing PEGs of a grade exceeding 3000 for the treatment or prevention of vaginal atrophy.