Mucoadhesive Polysaccharide Matrix for Prolonged API Residence

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Solution Overview

Problem

Current topical treatments for mucous membrane conditions face limitations due to short permeability and adhesion time, leading to reduced effectiveness and increased side effects from systemic medications, particularly in conditions like otitis, vaginal dryness, and mouth sores, where prolonged adhesion and controlled release of active pharmaceutical ingredients (APIs) are needed.

Innovation Solution

The development of mucoadhesive pharmaceutical compositions incorporating a synergistic combination of polysaccharide polymers such as amylopectin, pullulan, hyaluronic acid, and tamarind xyloglucan, which enhance the adhesion and release of APIs on mucous membranes, providing a prolonged residence time and controlled delivery of medications.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Duration of action of stationary object

If conventional topical treatments are used, then application is simple and immediate relief is achieved, but adhesion time is short and frequent dosing is required

Engineering Contradiction:
Improveadhesion timeVSAvoidformulation complexity
Core Design Contradiction:
Duration of action of stationary objectVSDevice complexity

Solution Approach 1:

The patent employs a composite mucoadhesive formulation combining multiple polysaccharide polymers (amylopectin, pullulan, hyaluronic acid, and xyloglucan) to achieve prolonged adhesion time. Each polymer contributes specific properties: amylopectin provides structural framework, pullulan ensures mucoadhesion, hyaluronic acid maintains hydration, and xyloglucan enhances binding strength. This composite approach resolves the contradiction by achieving extended residence time without excessive complexity through synergistic material combination.

Inventive Principle:
Principle #40Composite materials

Solution Approach 2:

The patent merges multiple polysaccharide polymers into a single integrated mucoadhesive matrix that works synergistically to extend adhesion time. The combination of amylopectin, pullulan, hyaluronic acid, and xyloglucan creates a unified structure that maintains stability and adhesion properties while reducing the need for frequent dosing, thus resolving the contradiction between prolonged action and formulation complexity.

Inventive Principle:
Principle #5Merging (Combining)

2Reliability

If oral medications are used, then systemic effectiveness is improved, but side effects increase due to systemic distribution

Engineering Contradiction:
Improvetreatment effectivenessVSAvoidsystemic side effects
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent applies local quality by creating a mucoadhesive formulation that remains localized at the site of application on mucous membranes. The polysaccharide-based matrix ensures the medication stays at the target location through prolonged adhesion, providing localized treatment effectiveness without the systemic distribution and associated side effects of oral medications. This directly resolves the contradiction between treatment reliability and harmful side effects.

Inventive Principle:
Principle #3Local quality

Solution Approach 2:

The polysaccharide polymer matrix acts as an intermediary carrier that facilitates localized delivery of the active pharmaceutical ingredient. This intermediary system ensures the medication remains at the application site through extended adhesion time, maintaining treatment effectiveness while preventing systemic absorption and associated side effects, thus resolving the contradiction between reliability and harmful factors.

Inventive Principle:
Principle #24Intermediary (Mediator)

3Reliability

If strong antibiotics are administered orally, then infection treatment effectiveness is improved, but microbial balance is disrupted causing fungal overgrowth

Engineering Contradiction:
Improveinfection treatment effectivenessVSAvoidmicrobial imbalance
Core Design Contradiction:
ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The patent applies local quality by delivering antibiotics through a mucoadhesive formulation that confines the medication to the specific site of infection on mucous membranes. This localized delivery maintains treatment effectiveness against the infection while minimizing systemic distribution that would disrupt microbial balance and cause fungal overgrowth. The polysaccharide matrix ensures the antibiotic remains at the target location, resolving the contradiction between treatment effectiveness and harmful microbial imbalance.

Inventive Principle:
Principle #3Local quality

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 mucoadhesive compositions significantly extend the adhesion time of APIs on mucous membranes, improving treatment efficacy and reducing the frequency of dosing, while minimizing systemic side effects by maintaining prolonged contact with the target site and ensuring safer, more effective localized delivery.

Implementation Method 1

The mucoadhesive compositions significantly extend the adhesion time of APIs on mucous membranes

Methodology Applied
Scientific EffectMucoadhesion: Adhesive

Implementation Method 2

improving the release of as well as the adhesion time of APIs

Methodology Applied
Scientific EffectControlled release: Diffusion

Data Source

PatentUS11623008B2Excipient compositions for mucoadhesive pharmaceutical compositions including a synergistic combination of amylopectin, pullulan, hyaluronic acid, and xyloglucan
Publication Date: 2023.04.11 PROFESSIONAL COMPOUNDING CENTS OF AMERICA PCCA
  • US11623008B2 patent drawing
  • US11623008B2 patent drawing
  • US11623008B2 patent drawing

AI summary

Excipient compositions including a combination of excipients for mucoadhesive pharmaceutical compositions that improve mucoadhesiveness power, as well as release of and adhesion time of suitable active pharmaceutical ingredients (APIs) are disclosed. The excipient compositions include an aqueous solution with a synergistic combination of polymers, such as, for example amylopectin, pullulan, hyaluronic acid, and tamarind xyloglucan, among others. These polymers have been demonstrated to improve the release of as well as the adhesion time of APIs onto mucosa membrane. Mucoadhesive pharmaceutical compositions that include excipient compositions include suitable APIs, such as, for example analgesics, anesthetics, anthelmintics, anti-allergic agents, anti-fungals, antihistamines, anti-inflammatory agents, antimigraine agents, and hormones, among others. Mucoadhesive pharmaceutical compositions including excipient compositions are employed in the treatment of a plurality of mucous membrane diseases.