Phospholipid Ear Drop Carriers for Otitis Externa

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Solution Overview

Problem

Current treatments for otitis externa, such as conventional ear drops, often fail to maintain medication in contact with the affected tissue long enough, especially in cases involving fungal or parasitic infestations, and can be uncomfortable due to their adhesive nature, leading to compliance issues and the need for frequent dosing.

Innovation Solution

A multiple agent composition using lipid-based carriers, such as liposomes, that can be applied topically without gelling agents or adhesives, allowing for a single or infrequent dose application to effectively treat otitis externa by maintaining the medication in the ear canal for an adequate duration.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Duration of action of moving object

If conventional ear drops are used to treat otitis externa, then the medication can be applied easily, but the medication cannot be maintained in contact with the affected tissue long enough

Engineering Contradiction:
Improveresidence time of medicationVSAvoidapplication convenience
Core Design Contradiction:
Duration of action of moving objectVSEase of operation

Solution Approach 1:

The patent changes the physical and chemical parameters of the ear drop formulation by incorporating specific excipients (hydroxyethylcellulose, glycerin, propylene glycol, and phospholipids) that modify the viscosity, adhesion, and retention properties of the medication, allowing it to remain in contact with affected tissue for extended periods without requiring gel or adhesive formulations

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent creates a composite ear drop formulation combining multiple components (active pharmaceutical ingredients, hydroxyethylcellulose, glycerin, propylene glycol, and phospholipids) that work synergistically to provide both easy application and prolonged residence time on the ear canal tissue

Inventive Principle:
Principle #40Composite materials

2Duration of action of moving object

If gels or adhesive formulations are used to increase medication residence time, then the medication can be retained in the ear, but the thick and sticky feel causes patient frustration and compliance issues

Engineering Contradiction:
Improveresidence time of medicationVSAvoidpatient compliance
Core Design Contradiction:
Duration of action of moving objectVSEase of operation

Solution Approach 1:

The patent optimizes the viscosity and rheological parameters of the ear drop formulation by carefully selecting and dosing excipients (0.5-5% hydroxyethylcellulose, 5-50% glycerin, 5-50% propylene glycol, 0.1-10% phospholipids) to achieve prolonged retention without creating a thick or sticky sensation that would bother patients

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The formulation provides localized adhesion and retention properties at the site of application in the ear canal while maintaining an overall fluid consistency that feels comfortable and non-sticky during application, allowing different regions of the formulation to serve different functions

Inventive Principle:
Principle #3Local quality

3Reliability

If oral antibiotics are used to treat otitis externa, then systemic distribution of the drug occurs, but this dilutes the medication and exposes the patient to side effects

Engineering Contradiction:
Improvetreatment efficacyVSAvoidside effects from systemic delivery
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent extracts the antibiotic or antifungal active ingredients from systemic oral administration and delivers them directly to the site of infection in the ear canal through topical ear drops, eliminating the need for systemic distribution and associated side effects while maintaining treatment efficacy

Inventive Principle:
Principle #2Taking out (Extraction)

Solution Approach 2:

The ear drop formulation acts as an intermediary delivery system that transports the active pharmaceutical ingredients directly to the affected ear canal tissue, bypassing the gastrointestinal tract and systemic circulation to achieve localized treatment with minimal systemic exposure

Inventive Principle:
Principle #24Intermediary (Mediator)

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

This approach enables significant reduction or complete resolution of otitis externa symptoms with minimal dosing, making it suitable for both treatment and prophylaxis, particularly effective in reducing the need for frequent applications and improving compliance, especially in animals and young children.

Implementation Method 1

A multiple agent composition using lipid-based carriers, such as liposomes, that can be applied topically without gelling agents or adhesives, allowing for a single or infrequent dose application to effectively treat otitis externa by maintaining the medication in the ear canal for an adequate duration

Methodology Applied
Scientific EffectLiposome encapsulation and delivery:

Data Source

PatentEP2498792B1Compositions comprising phospholipid carriers for the treatment of otitis externa
Publication Date: 2017.08.02 BAYER HEALTHCARE LLC
  • EP2498792B1 patent drawing
  • EP2498792B1 patent drawing

AI summary

Methods for treating and preventing otitis externa with a course of treatment consisting of as little as a single dose are provided. The methods are practiced by topical administration of compositions having a lipid carrier, such as liposomes and non- vesicular lipids, to the outer ear canal. Such compositions lack viscocity-enhancing celluloses or adhesives, and are preferably not in the form of a gel. Active agents useful for treating pain, inflammation, fungal or parasitic infestation and/or infections in the outer ear are co- administered in or with the composition.