Buccal Mucoadhesive Patch for Protein Release

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Solution Overview

Problem

The oral administration of proteins is challenging due to their sensitivity to gastrointestinal enzymes, and there is a need for a mucoadhesive system with optimized permeation capacity to reduce therapeutic doses and improve absorption control.

Innovation Solution

A mucoadhesive patch comprising multiple bilayers of chitosan and hyaluronic acid, designed for buccal or sublingual application, which adheres to the mucosa, allowing controlled release of proteins and peptides, and is self-supporting, dissolving in saliva to facilitate enzyme degradation.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of operation

If proteins are administered orally, then the administration route is simple and widely used, but the proteins are degraded by gastrointestinal enzymes and absorption is poor

Engineering Contradiction:
Improveadministration routeVSAvoidprotein stability
Core Design Contradiction:
Ease of operationVSReliability

Solution Approach 1:

The invention extracts the protein delivery system from the gastrointestinal tract environment and relocates it to the buccal cavity, where enzymes are absent. The mucoadhesive patch delivers proteins directly through the buccal mucosa, bypassing the harmful gastrointestinal enzymatic environment while maintaining simple administration.

Inventive Principle:
Principle #2Taking out (Extraction)

Solution Approach 2:

The mucoadhesive patch acts as an intermediary delivery system that enables protein transport across the buccal mucosa. It mediates between the protein cargo and the mucosal tissue, facilitating controlled release and absorption while protecting the protein from degradation.

Inventive Principle:
Principle #24Intermediary (Mediator)

2Reliability

If a mucoadhesive system is used for protein delivery, then absorption control is improved, but the permeation capacity needs optimization to reduce therapeutic dose

Engineering Contradiction:
Improveabsorption controlVSAvoidtherapeutic dose
Core Design Contradiction:
ReliabilityVSQuantity of substance

Solution Approach 1:

The invention optimizes the mucoadhesive system by adjusting key parameters: using specific polysaccharide combinations (chitosan and hyaluronic acid) with controlled molecular weights, optimizing bilayer structure and thickness, and tuning the mucoadhesive strength to achieve ideal balance between retention time and permeation capacity, thereby reducing the required therapeutic dose.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patch employs a composite structure combining chitosan and hyaluronic acid bilayers. This composite material system provides enhanced mucoadhesion, controlled permeation, and optimized drug release profile, allowing for reduced therapeutic doses while maintaining effective absorption control.

Inventive Principle:
Principle #40Composite materials

3Reliability

If multiple bilayers are used in the patch, then controlled release and permeation are improved, but the device complexity increases

Engineering Contradiction:
Improvecontrolled releaseVSAvoidpatch structure
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patch is segmented into multiple thin bilayer units (chitosan-hyaluronic acid repeats), where each layer contributes specific functions. This segmentation allows controlled release through the layered structure while maintaining a relatively simple overall design that can be fabricated using straightforward layer-by-layer assembly techniques.

Inventive Principle:
Principle #1Segmentation

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 provides controlled and efficient absorption of proteins, maintaining bioactivity and avoiding inflammation, with prolonged retention and penetration into the mucosa, effectively reducing the therapeutic dose required.

Implementation Method 1

forming a CHI/anionic polysaccharide multilayer membrane by a method of layer by layer deposition on a substrate

Methodology Applied
Scientific EffectLayer by layer deposition: Deposition (physical)

Implementation Method 2

The patch adheres to the buccal or sublingual mucosa

Methodology Applied
Scientific EffectMucoadhesion: Adhesive

Implementation Method 3

said protein or said polypeptide being incorporated in said patch and/or adsorbed on the surface of said patch

Methodology Applied
Scientific EffectAdsorption: Adsorption

Implementation Method 4

The patch is self-supporting and dissolves in the saliva owing to the presence of enzymes capable of degrading the two polysaccharides

Methodology Applied
Scientific EffectEnzymatic degradation: Enzyme

Data Source

PatentUS20230405113A1Systems for buccal release of proteins
Publication Date: 2023.12.21 CENT NAT DE LA RECH SCI (C N R S)
  • US20230405113A1 patent drawing
  • US20230405113A1 patent drawing
  • US20230405113A1 patent drawing

AI summary

The present invention relates to a mucoadhesive patch for buccal or sublingual release of a protein or polypeptide, said patch comprising at least 100 bilayers each composed of a layer of chitosan (CHI) and a layer of an anionic polysaccharide. The invention also relates to a method for producing such a patch.