Compressed Chitosan Mucoadhesive Matrix for pH-Resistant Drug Delivery

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Solution Overview

Problem

Conventional chitosan-based mucoadhesive preparations lose their adhesive properties at physiological pH, leading to inadequate mucoadhesion and shorter residence times, and often require harsh chemical crosslinking agents, which can damage thermally unstable drugs and result in premature drug release.

Innovation Solution

A compressed mucoadhesive preparation comprising unmodified chitosan and an organic acid, where chitosan is contacted with the acid, lyophilized, and then compressed to form a porous matrix that maintains mucoadhesive characteristics at physiological pH, preventing swelling and ensuring prolonged drug release.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional chitosan preparations are used, then mucoadhesive properties are achieved at acidic pH, but mucoadhesion is lost at physiological pH due to deprotonation

Engineering Contradiction:

Improvemucoadhesive propertiesVSAvoidpH adaptability

Core Design Contradiction:

ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent changes the physical state parameter of chitosan from soluble to compressed porous form, which maintains the cationic charge and mucoadhesive properties at physiological pH without requiring chemical modification

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The patent creates a composite structure by compressing chitosan into a porous matrix that combines the benefits of chitosan's mucoadhesion with a stable physical form that prevents pH-induced deprotonation

Inventive Principle:

Principle #40Composite materials

2Reliability

If chemical crosslinking agents are used to improve stability, then mucoadhesive characteristics are enhanced, but thermally unstable drugs are damaged

Engineering Contradiction:

Improvemucoadhesive characteristicsVSAvoiddrug degradation

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent extracts and eliminates the harmful chemical crosslinking agents from the formulation, achieving stability through the physical compressed porous structure of chitosan instead

Inventive Principle:

Principle #2Taking out (Extraction)

Solution Approach 2:

The compressed porous structure acts as an intermediary that provides mechanical stability and controlled release without requiring harsh chemical agents that would damage sensitive drugs

Inventive Principle:

Principle #24Intermediary (Mediator)

3Duration of action of moving object

If conventional chitosan formulations are used, then drug delivery is achieved, but residence time at application sites is short due to charge neutralization

Engineering Contradiction:

Improveresidence timeVSAvoidmucoadhesion

Core Design Contradiction:

Duration of action of moving objectVSReliability

Solution Approach 1:

The patent changes the physical form parameter to compressed porous structure, which maintains the cationic charge density and prevents neutralization by physiological secretions, thereby extending residence time

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The chitosan is pre-compressed into a porous matrix before application, which stabilizes the cationic charge and prepares the structure for prolonged mucoadhesion at the application site

Inventive Principle:

Principle #10Preliminary action

4Productivity

If fluid absorption and swelling is allowed, then drug release occurs, but the patch becomes bulky and may get dislodged

Engineering Contradiction:

Improvedrug releaseVSAvoidadhesion stability

Core Design Contradiction:

ProductivityVSReliability

Solution Approach 1:

The patent uses a compressed porous structure that allows controlled drug release through the pores without causing excessive swelling, maintaining a thin profile and stable adhesion

Inventive Principle:

Principle #31Porous materials

Solution Approach 2:

The patent changes the density and porosity parameters by compressing the chitosan, creating a structure that permits drug release while preventing excessive fluid absorption and swelling

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 solution provides sustained and controlled drug delivery with enhanced mucoadhesion time, preventing premature drug release and maintaining stability, even with thermally labile drugs, while avoiding the use of harsh chemicals.

Implementation Method 1

The primary amine in the glucosamine units of chitosan undergoes protonation in acidic pH and renders a highly cationic charge to the chitosan chains

Methodology Applied

Scientific EffectProtonation:

Implementation Method 2

subjecting the chitosan solution to lyophilisation to obtain dry chitosan sponge

Methodology Applied

Scientific EffectLyophilisation: Freeze Drying

Implementation Method 3

compressing the dry chitosan sponge to obtain a mucoadhesive preparation

Methodology Applied

Scientific EffectCompression: Compression

Implementation Method 4

enhanced mucoadhesive characteristics and sustained drug release... preventing swelling

Methodology Applied

Scientific EffectMucoadhesion: Adhesive

Data Source

PatentUS11491107B2Mucoadhesive preparations, methods and applications thereof

Publication Date: 2022.11.08 AXIO BIOSOLUTIONS PVT

AI summary

The present disclosure relates to mucoadhesive preparation comprising chitosan, and methods thereof. Further, the present disclosure relates to applications of the mucoadhesive preparation.