Biodegradable Ocular Implant Sustained Drug Release

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Solution Overview

Problem

Current glaucoma therapies have low compliance and are associated with local and systemic side effects due to fluctuations in intraocular pressure, leading to increased costs and faster disease progression, with no FDA-approved sustained-release therapies directly targeting the anterior chamber of the eye.

Innovation Solution

Development of a biodegradable sustained-release pharmaceutical formulation using PRINT technology for ocular implants with precise engineering, providing uniform size, shape, and drug distribution, containing prostaglandin analogues like travoprost, to treat elevated intraocular pressure and glaucoma.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If topical ophthalmic agents are used to treat glaucoma, then intraocular pressure is reduced, but compliance is low and side effects occur due to drug level fluctuations

Engineering Contradiction:
ImprovecomplianceVSAvoiddrug level stability
Core Design Contradiction:
ReliabilityVSEase of operation

Solution Approach 1:

The implant is pre-loaded with therapeutic agent in a biodegradable polymer matrix before insertion into the anterior chamber. This preliminary preparation allows the implant to immediately begin sustained release upon placement, eliminating the need for repeated patient administration actions and ensuring consistent drug levels from the start of treatment.

Inventive Principle:
Principle #10Preliminary action

Solution Approach 2:

The biodegradable polymer matrix provides continuous sustained release of the therapeutic agent over an extended period (e.g., 6 months to 1 year). This continuous release mechanism maintains stable drug levels in the aqueous humor, eliminating the peak-and-trough fluctuations associated with topical administration and ensuring uninterrupted therapeutic action.

Inventive Principle:
Principle #20Continuity of useful action

2Reliability

If topical ophthalmic agents are administered frequently, then intraocular pressure control is maintained, but side effects increase due to peak drug levels

Engineering Contradiction:
Improveintraocular pressure controlVSAvoidside effects
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The implant delivers the therapeutic agent at a steady, controlled rate over an extended period, avoiding the peak drug levels that occur with frequent topical administration. This continuous low-level release maintains effective intraocular pressure control while minimizing concentration-dependent side effects such as hyperemia and orbital fat atrophy.

Inventive Principle:
Principle #20Continuity of useful action

Solution Approach 2:

The formulation changes the drug delivery parameters by using a biodegradable polymer matrix with specific degradation kinetics. This transforms the administration pattern from frequent high-concentration doses to a single implantation followed by sustained low-concentration release, altering the pharmacokinetic profile to reduce side effects while maintaining therapeutic efficacy.

Inventive Principle:
Principle #35Parameter changes

3Reliability

If sustained-release implant is developed, then compliance and safety are improved, but manufacturing complexity increases

Engineering Contradiction:
Improvesafety profileVSAvoidmanufacturing process
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The manufacturing process controls critical parameters such as polymer molecular weight, drug-polymer ratio, and particle size distribution to achieve the desired sustained release profile. By precisely controlling these parameters during formulation and fabrication, the implant achieves reliable safety and efficacy without requiring overly complex manufacturing steps.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The implant uses a composite structure combining a biodegradable polymer matrix with the therapeutic agent. This composite approach allows the polymer to provide both the structural framework and the controlled release mechanism, simplifying the overall device design while achieving the desired sustained release performance and safety profile.

Inventive Principle:
Principle #40Composite materials

4Ease of operation

If implant size is reduced for easier insertion, then delivery becomes easier, but drug loading capacity decreases

Engineering Contradiction:
Improveinsertion easeVSAvoiddrug loading capacity
Core Design Contradiction:
Ease of operationVSQuantity of substance

Solution Approach 1:

The formulation optimizes the drug loading concentration within the polymer matrix to achieve adequate total drug capacity in a small implant volume. By adjusting parameters such as drug-polymer ratio and polymer crosslinking density, the implant maintains sufficient therapeutic agent load while keeping dimensions small enough for easy insertion through standard ophthalmic instruments.

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 biodegradable ocular implants offer improved compliance and safety by maintaining a consistent drug release profile, reducing intraocular pressure effectively and minimizing side effects, thus potentially slowing glaucoma progression.

Implementation Method 1

a sustained release pharmaceutical formulation administered directly to the anterior chamber of an eye

Methodology Applied
Scientific EffectDiffusion: Diffusion

Implementation Method 2

biodegradable polymer matrix that contains a homogenously dispersed therapeutic agent therein

Methodology Applied
Scientific EffectBiodegradation: Decomposition (biological)

Data Source

PatentEP3076948B1Intracameral implant for treatment of an ocular condition
Publication Date: 2020.11.18 ALLERGAN INC
  • EP3076948B1 patent drawingFigure 1
  • EP3076948B1 patent drawingFigure 2A
  • EP3076948B1 patent drawingFigure 2B

AI summary

The disclosure teaches precisely engineered biodegradable drug delivery systems and methods of making and utilizing such systems. In aspects, the biodegradable drug delivery systems taught herein comprise ocular implants having a desired extended drug release profile suitable for treating elevated intraocular pressure.