Transdermal Adjuvant Patch for Safe Immune Response

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Solution Overview

Problem

Conventional adjuvants used in vaccinations often cause local tissue damage and have poor skin permeability, making them unsuitable for transdermal administration, and existing methods for enhancing immune responses through transdermal delivery are inefficient and costly.

Innovation Solution

A pharmaceutical preparation comprising a low molecular weight adjuvant, such as lauryl alcohol, combined with an antigen in a patch form using an adhesive like acrylic copolymer or rubber polymer, which can be applied transdermally or transmucosally without causing skin irritation, enhancing immunogenicity and allowing for efficient antigen delivery.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional adjuvants (aluminum compounds, ISCOM, bacterial derivatives) are administered subcutaneously or intramuscularly, then immune response enhancement is achieved, but local tissue damage occurs (contact hypersensitivity, granuloma formation, erythema)

Engineering Contradiction:
Improveimmune response enhancementVSAvoidlocal tissue damage
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent uses liposomes as intermediary carriers to deliver adjuvants (such as TLR agonists) and antigens transdermally. The liposome structure protects the adjuvant from direct contact with tissues while facilitating controlled release through the skin barrier, thereby enhancing immune response without causing local tissue damage associated with conventional injection methods

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent replaces the mechanical injection system (needles, syringes) with a transdermal delivery system using liposomal formulations. This substitution eliminates the need for parenteral administration while achieving equivalent or superior immune stimulation through skin penetration, avoiding the tissue trauma inherent in injection methods

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

2Object-affected harmful factors

If conventional adjuvants are administered transdermally to avoid tissue damage, then safety is improved, but skin permeability is poor and absorption is limited

Engineering Contradiction:
Improvetissue damage avoidanceVSAvoidadjuvant absorption
Core Design Contradiction:
Object-affected harmful factorsVSQuantity of substance

Solution Approach 1:

The patent modifies the physical and chemical parameters of adjuvants by encapsulating them in liposomes. This encapsulation changes the adjuvant's solubility, stability, and penetration properties, enabling transdermal delivery. The liposomal formulation allows controlled release and enhances absorption through the skin barrier while maintaining safety

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent creates composite delivery systems combining liposomes with adjuvants and antigens. This composite structure integrates the benefits of liposomal protection and delivery with the immunogenic properties of the adjuvant, achieving both safe transdermal administration and sufficient absorption to enhance immune response

Inventive Principle:
Principle #40Composite materials

3Reliability

If macromolecular adjuvants (ISCOM, bacterial derivatives) are used, then immune stimulation is achieved, but transdermal absorbability is poor and dosing frequency increases

Engineering Contradiction:
Improveimmune stimulationVSAvoiddosing frequency
Core Design Contradiction:
ReliabilityVSLoss of time

Solution Approach 1:

The patent segments macromolecular adjuvants into smaller liposomal units that can be effectively delivered transdermally. By dividing the adjuvant into manageable liposomal carriers, the system achieves both immune stimulation and improved transdermal penetration, reducing the need for frequent dosing

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The patent achieves continuous immune stimulation through sustained release of adjuvants from liposomal formulations. The liposomes provide prolonged release of the immunostimulatory agent, maintaining effective concentrations over extended periods and reducing dosing frequency while ensuring continuous immune activation

Inventive Principle:
Principle #20Continuity of useful action

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 patch preparation effectively enhances antigen immunogenicity without skin irritation, enabling quicker and longer-term delivery of the adjuvant, reducing the need for frequent dosing and improving immune responses in vulnerable populations like seniors and immunocompromised individuals, while being cost-effective.

Implementation Method 1

Langerhans cells capture a protein antigen that invades into skin, disintegrate it inside and express a peptide fragment on an MHC molecule

Methodology Applied
Scientific EffectPhagocytosis:

Implementation Method 2

An adjuvant is a substance that enhances immunogenicity, and when it is administered together with an antigen, a response thereof to the antigen is enhanced

Methodology Applied
Scientific EffectAdjuvant effect:

Implementation Method 3

the stratum corneum consisting of the dead cell layer and lipid bilayers shows a strong barrier function for many substances

Methodology Applied
Scientific EffectBarrier function:

Data Source

PatentEP2123296B1Adjuvant for transdermal or transmucosal administration and pharmaceutical preparation containing the same
Publication Date: 2019.05.22 HISAMITSU PHARM CO INC
  • EP2123296B1 patent drawingFigure 1~2
  • EP2123296B1 patent drawingFigure 3~4
  • EP2123296B1 patent drawingFigure 5~6

AI summary

It is intended to provide 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 enhancing immunogenicity of an antigen efficiently. It can be achieved by an immunostimulant adjuvant containing at least one substance selected from the group consisting of aliphatic alcohols, free fatty acids and fatty acid derivatives but does not contain a substance represented by the following formula. (In the formula, R3 and R4 may be combined to form a cyclic ring, and R1 and R2 independently represent an alkyl side chain having 1 to 16 carbon atoms.)