Biodegradable Ocular Insert Sustaining Dexamethasone Release

Solution Overview

Problem

Current treatments for dry eye disease (DED) face challenges such as short-term efficacy, frequent administration of glucocorticoid eye drops leading to high concentrations and safety issues, tolerability problems like burning and stinging, and poor patient compliance due to complexity and accuracy concerns in drop delivery.

Innovation Solution

A biodegradable ocular insert containing dexamethasone for sustained release into the tear fluid, administered in the superior and/or inferior canaliculus, providing a controlled and prolonged anti-inflammatory effect without daily administration, designed to be easy to handle and secure, reducing side effects and improving compliance.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If glucocorticoid eye drops are administered multiple times per day to maintain therapeutic levels, then the anti-inflammatory effect is improved, but the risk of high peak concentrations and safety issues increases

Engineering Contradiction:

Improveanti-inflammatory effectVSAvoidpeak concentrations and safety issues

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The insert is pre-loaded with a controlled amount of glucocorticoid that is released gradually over time. This preliminary preparation allows the therapeutic agent to be delivered continuously without requiring multiple daily administrations, thereby avoiding peak concentrations while maintaining effective anti-inflammatory levels throughout the treatment period.

Inventive Principle:

Principle #10Preliminary action

Solution Approach 2:

The ocular insert provides continuous release of the glucocorticoid over an extended period (e.g., 7-14 days), eliminating the need for intermittent dosing. This continuous delivery mechanism maintains stable therapeutic concentrations in the tear film, avoiding the peak-trough fluctuations associated with multiple daily drops while ensuring sustained anti-inflammatory effect.

Inventive Principle:

Principle #20Continuity of useful action

2Quantity of substance

If ophthalmic drops are administered several times per day to compensate for quick washing out, then therapeutic exposure is improved, but patient compliance decreases due to frequent administration

Engineering Contradiction:

Improvetotal exposure to active agentVSAvoidpatient compliance

Core Design Contradiction:

Quantity of substanceVSEase of operation

Solution Approach 1:

The insert is pre-loaded with a controlled amount of glucocorticoid that is released gradually over time. This preliminary preparation allows the therapeutic agent to be delivered continuously without requiring multiple daily administrations, thereby avoiding peak concentrations while maintaining effective anti-inflammatory levels throughout the treatment period.

Inventive Principle:

Principle #10Preliminary action

Solution Approach 2:

The ocular insert provides continuous release of the glucocorticoid over an extended period (e.g., 7-14 days), eliminating the need for intermittent dosing. This continuous delivery mechanism maintains stable therapeutic concentrations in the tear film, avoiding the peak-trough fluctuations associated with multiple daily drops while ensuring sustained anti-inflammatory effect.

Inventive Principle:

Principle #20Continuity of useful action

3Reliability

If high concentration formulations are used to compensate for short exposure time from drop administration, then therapeutic effect is improved, but adverse effects from acute high concentrations may occur

Engineering Contradiction:

Improvetherapeutic effectVSAvoidadverse effects from acute high concentrations

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The invention changes the delivery parameters from high concentration/short duration (eye drops) to low concentration/long duration (insert). The insert releases the glucocorticoid at a controlled, lower rate over an extended period, maintaining adequate therapeutic exposure while avoiding acute peak concentrations that cause adverse effects. This parameter transformation resolves the contradiction between therapeutic effectiveness and safety.

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 ocular insert offers a sustained, effective treatment of DED symptoms for up to several weeks with a single administration, reducing side effects and improving patient compliance by maintaining therapeutic levels of dexamethasone in the tear film, minimizing systemic absorption, and avoiding peak concentrations that could cause adverse effects.

Implementation Method 1

A biodegradable ocular insert containing dexamethasone for sustained release into the tear fluid

Methodology Applied

Scientific EffectBiodegradation: Decomposition (biological)

Data Source

PatentUS20220183969A1Ocular insert containing a glucocorticoid

Publication Date: 2022.06.16 OCULAR THERAPEUTIX INC

AI summary

In certain embodiments, the invention relates to a sustained release biodegradable intracanalicular insert containing a glucocorticoid dispersed in a hydrogel for the treatment of dry eye disease.