Segmented Bioerodible Implants for Ocular Drug Delivery

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Solution Overview

Problem

Current drug delivery systems for ocular conditions face challenges in achieving sustained therapeutic levels in the eye, leading to systemic side effects and frequent injections due to short intraocular half-lives of active agents, and they struggle with flexible drug release profiles and 'drug holidays', necessitating multiple interventions.

Innovation Solution

The development of segmented bioerodible implants using poly(lactide) and poly(lactide-co-glycolide) copolymers with different polymer blends and excipients to provide independent and flexible drug release profiles, allowing for extended release of therapeutic agents over 3 to 6 months with optional 'drug holidays', minimizing systemic side effects and interventions.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Duration of action of moving object

If current drug delivery systems are used for ocular conditions, then frequent injections are required due to short intraocular half-lives, but this increases the frequency of interventions and procedural burden

Engineering Contradiction:
Improveintraocular half-lifeVSAvoidfrequency of interventions
Core Design Contradiction:
Duration of action of moving objectVSProductivity

Solution Approach 1:

The implant is divided into multiple segments that can separate in situ after implantation. Each segment contains drug and polymer in different ratios, creating independent release profiles that collectively provide extended sustained release over 3-6 months, eliminating the need for frequent injections

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

Different segments are formulated with varying drug-to-polymer ratios and excipient compositions to create localized quality differences. This allows each segment to release drug at different rates, providing flexible and adjustable release profiles tailored to therapeutic needs while maintaining extended duration of action

Inventive Principle:
Principle #3Local quality

2Reliability

If current drug delivery systems are used, then systemic side effects occur due to lack of sustained therapeutic levels, but achieving sustained levels requires multiple interventions

Engineering Contradiction:
Improvesustained therapeutic levelsVSAvoidmultiple interventions
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The segmented implant structure allows each segment to contribute to sustained therapeutic levels through independent release kinetics. The collective action of multiple segments with different release profiles ensures reliable maintained drug levels in the eye for extended periods, avoiding systemic side effects while requiring only a single implantation procedure

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The implant segments are designed to release drug continuously over 3-6 months through controlled polymer erosion and diffusion. This continuous release mechanism maintains reliable therapeutic levels throughout the ocular tissue, eliminating the need for repeated interventions to achieve and maintain effective drug concentrations

Inventive Principle:
Principle #20Continuity of useful action

3Adaptability or versatility

If single-profile drug release is used, then flexible drug release profiles and drug holidays cannot be achieved, but achieving extended release requires complex multiple interventions

Engineering Contradiction:
Improvedrug release profilesVSAvoidnumber of interventions
Core Design Contradiction:
Adaptability or versatilityVSProductivity

Solution Approach 1:

The implant is segmented into multiple independent units that can be formulated with different drug-to-polymer ratios and excipient compositions. This segmentation enables each segment to have a unique release profile, providing flexibility to tailor drug release patterns (sustained, delayed, pulsed) while achieving extended release through a single implantation procedure

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

Different segments are engineered with localized quality variations including different polymer blends (poly(lactide), poly(lactide-co-glycolide)), varying drug concentrations, and different excipients. This allows customization of release profiles for each segment, enabling flexible drug delivery strategies such as drug holidays or pulsed release without requiring multiple separate interventions

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

This approach enables sustained therapeutic levels in the eye for extended periods, reducing systemic side effects and the frequency of interventions by providing flexible and adjustable drug release profiles, effectively managing ocular conditions such as macular degeneration and uveitis.

Implementation Method 1

each segment comprising an active agent and a bioerodible polymer... varying and extended release rates to provide for improved kinetics of release

Methodology Applied
Scientific EffectHydrolysis: Hydrolysis

Implementation Method 2

release a therapeutic level of the active agent into the ocular region or site for a period time between about 30 days and about 1 year

Methodology Applied
Scientific EffectDiffusion: Diffusion

Data Source

PatentUS8956655B2Biodegradable drug delivery system
Publication Date: 2015.02.17 ALLERGAN INC
  • US8956655B2 patent drawing

AI summary

A drug delivery system (DDS) comprised of segmented biodegradable implants sized and suitable for implantation in an ocular region or site and methods for treating ocular conditions. The segmented implants provide an extended release of an active agent at a therapeutically effective amount for a period of time between 50 days and one year, or longer, and permit the DDS to have segments that possess individual and different drug release characteristics.