Thermoreversible Gel for Inner Ear Drug Delivery

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Solution Overview

Problem

Current treatments for inner ear diseases face challenges such as limited delivery of active agents due to the blood-labyrinth barrier, osmotic imbalances, infections, and structural damage, leading to hearing loss and other complications.

Innovation Solution

A sterile, controlled release intratympanic composition comprising a neurotrophic growth factor as an aural pressure modulating agent, combined with a polyoxyethylene-polyoxypropylene triblock copolymer (Poloxamer 407) in a thermoreversible gel form, designed to provide sustained release for at least 3 days and maintain the ionic balance of inner ear fluids.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If active agents are administered to treat inner ear diseases, then treatment efficacy is improved, but delivery is limited due to the blood-labyrinth barrier

Engineering Contradiction:
Improvetreatment efficacyVSAvoiddelivery of active agent
Core Design Contradiction:
ReliabilityVSQuantity of substance

Solution Approach 1:

The patent uses the round window membrane as an intermediary pathway to bypass the blood-labyrinth barrier. By administering compositions through the round window, active agents can reach the inner ear without crossing the restrictive BLB, thereby improving delivery quantity while maintaining treatment efficacy

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent employs controlled release formulations that modify the release parameters of active agents over time. This sustained release mechanism ensures adequate drug concentration reaches the inner ear despite the barrier, resolving the contradiction between delivery quantity and treatment efficacy

Inventive Principle:
Principle #35Parameter changes

2Duration of action of moving object

If sustained release composition is used, then duration of action is improved, but complexity of formulation is increased

Engineering Contradiction:
Improveduration of releaseVSAvoidformulation complexity
Core Design Contradiction:
Duration of action of moving objectVSDevice complexity

Solution Approach 1:

The patent utilizes phase transition properties of poloxamer 407, which transitions from liquid at lower temperatures to gel at body temperature. This natural phase change enables sustained release functionality without complex mechanical structures, achieving extended duration of action while keeping the formulation relatively simple

Inventive Principle:
Principle #36Phase transitions

Solution Approach 2:

The patent combines poloxamer 407 with neurotrophic growth factors to create a composite formulation. The poloxamer provides the sustained release matrix while the growth factor provides the therapeutic action, achieving extended duration through material composition rather than complex device design

Inventive Principle:
Principle #40Composite materials

3Quantity of substance

If intratympanic composition is administered, then direct delivery to inner ear is improved, but risk of osmotic imbalance and infection is increased

Engineering Contradiction:
Improvedelivery to inner earVSAvoidosmotic imbalance and infection
Core Design Contradiction:
Quantity of substanceVSObject-affected harmful factors

Solution Approach 1:

The patent carefully controls the osmolarity parameter of the composition to match physiological conditions, preventing osmotic imbalance. The formulation is designed with specific osmolarity ranges that are isotonic to inner ear fluids, allowing direct delivery while eliminating the harmful effect of osmotic disruption

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent employs sterile techniques and preservatives to create a microenvironment that prevents microbial contamination. By maintaining an inert, sterile formulation environment, the composition can be administered directly to the inner ear through the round window without introducing infection risk

Inventive Principle:
Principle #39Inert atmosphere (Inert environment)

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 composition effectively delivers the active agent to the inner ear, reducing the risk of osmotic imbalances and infections, while providing prolonged exposure to the neurotrophic growth factor, thereby improving treatment efficacy and patient compliance.

Implementation Method 1

the composition is an auris-acceptable thermoreversible gel

Methodology Applied
Scientific EffectThermoreversible gel: Gel

Implementation Method 2

the composition provides sustained release of the aural pressure modulating agent into the inner ear for a period of at least 3 days

Methodology Applied
Scientific EffectControlled release:

Implementation Method 3

sterile water, q.s., buffered to provide a perilymph-suitable pH between about 6.0 and about 7.6

Methodology Applied
Scientific EffectpH buffering:

Implementation Method 4

between about 0.1 mg/mL to about 70 mg/mL of an aural pressure modulating agent, wherein the aural pressure modulating agent is a neurotrophic growth factor

Methodology Applied
Scientific EffectAural pressure modulation:

Data Source

PatentEP2278999B1Auris formulations for treating otic diseases and conditions
Publication Date: 2025.01.29 DOMPE FARMACEUTICI SPA
  • EP2278999B1 patent drawingFigure 1
  • EP2278999B1 patent drawingFigure 2
  • EP2278999B1 patent drawingFigure 3

AI summary

Disclosed herein are compositions and methods for the treatment of otic disorders with immunomodulating agents and auris pressure modulators. In these methods, the auris compositions and formulations are administered locally to an individual afflicted with an otic disorder, through direct application of the immunomodulating and/or auris pressure modulating compositions and formulations onto the auris media and/or auris interna target areas, or via perfusion into the auris media and/or auris interna structures.