Polyhydric Alcohol Adjuvants for Transdermal Immune Activation

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Solution Overview

Problem

Conventional adjuvants used for injection often cause local tissue damage and have poor skin permeability, making them unsuitable for transdermal or transmucosal administration, and there is a lack of effective, low molecular weight adjuvants that can enhance immunogenicity without skin irritation.

Innovation Solution

The use of polyhydric alcohols such as glycerin and propylene glycol, administered at high concentrations in various pharmaceutical preparations, including ointments and patches, to enhance immune activity transdermally or transmucosally, avoiding skin irritation and tissue damage.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional adjuvants (aluminum salts, ISCOMs, bacterial derivatives) are administered subcutaneously or intramuscularly, then immune response enhancement is achieved, but local tissue damage occurs

Engineering Contradiction:

Improveimmune response enhancementVSAvoidlocal tissue damage

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The invention changes the molecular weight parameter of adjuvants from macromolecular (conventional) to low molecular weight (new), enabling transdermal penetration while maintaining adjuvant activity. This parameter change resolves the contradiction by allowing safe transdermal administration that avoids the tissue damage associated with parenteral routes

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The invention introduces low molecular weight adjuvants as intermediary substances that can penetrate the skin barrier and activate Langerhans cells without causing tissue damage. These intermediaries bridge the gap between safe transdermal administration and effective immune stimulation

Inventive Principle:

Principle #24Intermediary (Mediator)

2Object-affected harmful factors

If conventional adjuvants are administered transdermally to avoid tissue damage, then safety is improved, but transdermal absorbability is poor

Engineering Contradiction:

Improveskin irritation and tissue damageVSAvoidtransdermal absorbability

Core Design Contradiction:

Object-affected harmful factorsVSQuantity of substance

Solution Approach 1:

The invention changes the molecular size parameter from macromolecular to low molecular weight, which fundamentally improves transdermal penetration capability. Low molecular weight substances can pass through the stratum corneum and reach Langerhans cells in the epidermis, resolving the absorbability problem

Inventive Principle:

Principle #35Parameter changes

3Reliability

If macromolecular adjuvants (ISCOMs, bacterial derivatives) are used, then adjuvant activity is achieved, but transdermal penetration is insufficient

Engineering Contradiction:

Improveadjuvant activityVSAvoidmolecular size for transdermal penetration

Core Design Contradiction:

ReliabilityVSLength of moving object

Solution Approach 1:

The invention changes the molecular weight parameter from macromolecular to low molecular weight, enabling transdermal penetration. The low molecular weight adjuvants can diffuse through the skin barrier while maintaining their ability to activate Langerhans cells and enhance immune responses

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The invention extracts the essential adjuvant activity from macromolecular structures and concentrates it in low molecular weight forms. By taking out the core immunostimulatory function and removing the bulky molecular structure, the adjuvant becomes penetrable while retaining efficacy

Inventive Principle:

Principle #2Taking out (Extraction)

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

Glycerin and propylene glycol demonstrate strong immunoenhancing effects with high safety and transdermal absorbability, providing excellent adjuvant activity without skin irritation, allowing for independent administration and flexible application routes, reducing the need for antigen dose considerations and minimizing site swelling and pain.

Implementation Method 1

certain low molecular compounds, in particular polyhydric alcohols such as glycerin as well as derivative thereof, not only show a strong immunoenhancing action, but also avoid skin irritation and tissue damage in transdermal or transmucosal administration

Methodology Applied

Scientific EffectTransdermal absorption: Absorption (physical)

Data Source

PatentEP2679242B1Adjuvant for transdermal or transmucosal administration and pharmaceutical preparation containing same

Publication Date: 2020.09.09 HISAMITSU PHARM CO INC

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AI summary

The present invention addresses the problem of providing a low-molecular weight adjuvant which can be administered safely without inducing skin irritation or the like by transdermal or transmucosal administration and is for efficiently enhancing the immunogenicity of an antigen. The present invention relates to an adjuvant for transdermal or transmucosal administration, containing at least one member selected from polyhydric alcohols and derivatives thereof including glycerol, glycerol derivatives and the like.