Redox-Responsive Polydopamine Nanoparticles for Ocular Drug Delivery

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Solution Overview

Problem

Current treatments for ophthalmological disorders, such as age-related macular degeneration, face challenges in delivering therapeutics effectively due to the delicate nature of the eye and limitations in addressing both anti-angiogenesis and anti-oxidization pathways, leading to side effects and reduced efficacy.

Innovation Solution

Development of redox-responsive ocular therapeutic compositions comprising polydopamine nanoparticles bound to anti-VEGF agents, which release therapeutics in response to increased reactive oxygen species, providing sustained and controlled drug delivery through erosion and degradation, tailored to the disease state.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If monthly intravitreal injection of anti-angiogenic therapeutics is used to treat wet AMD, then anti-angiogenesis effect is achieved, but treatment frequency and side effects increase

Engineering Contradiction:
Improveanti-angiogenesis efficacyVSAvoidside effects from repeated injections
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent applies preliminary action by pre-loading anti-VEGF therapeutics onto polydopamine nanoparticles before administration. The nanoparticles are prepared in advance with the therapeutic agent, allowing for sustained release over time rather than requiring repeated monthly injections. This preliminary preparation enables the therapeutic to be delivered in a single administration while maintaining efficacy over an extended period, thereby reducing the frequency of injections and associated side effects.

Inventive Principle:
Principle #10Preliminary action

Solution Approach 2:

The patent implements dynamics through the redox-responsive release mechanism of the polydopamine nanoparticles. The nanoparticles dynamically adjust their drug release rate based on the oxidative stress environment in the eye. When oxidative stress increases (indicated by higher ROS levels), the nanoparticles accelerate therapeutic release. This dynamic response allows the system to adapt to changing disease states, providing sustained anti-angiogenesis efficacy while reducing the need for repeated manual injections and their associated side effects.

Inventive Principle:
Principle #15Dynamics

2Reliability

If current anti-angiogenic treatments are used, then choroidal angiogenesis is inhibited, but intraocular oxidative stress is not alleviated

Engineering Contradiction:
Improveanti-angiogenesis efficacyVSAvoidintraocular oxidative stress
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent applies universality by designing polydopamine nanoparticles that perform multiple functions simultaneously. The nanoparticles serve as both a delivery vehicle for anti-VEGF therapeutics (anti-angiogenesis function) and as a source of antioxidants (oxidative stress alleviation function). The polydopamine material itself possesses antioxidant properties that can scavenge ROS, while also providing a platform for therapeutic delivery. This multi-functionality allows a single treatment to address both choroidal angiogenesis and intraocular oxidative stress, resolving the limitation of current monofunctional treatments.

Inventive Principle:
Principle #6Universality (Multi-functionality)

Solution Approach 2:

The patent converts the harmful effect of oxidative stress into a beneficial trigger for therapeutic release. The elevated ROS levels, which are harmful in themselves, serve as a signal that triggers accelerated release of the anti-angiogenic therapeutic from the nanoparticles. This redox-responsive mechanism transforms the harmful oxidative environment into a useful trigger that ensures the therapeutic is released precisely when and where it is most needed, while the polydopamine simultaneously mitigates the harmful oxidative stress through its antioxidant properties.

Inventive Principle:
Principle #22Blessing in disguise (Convert harm into benefit)

3Duration of action of moving object

If nanoparticle-based devices are used for sustained delivery, then delivery duration is extended, but redox-responsive controlled release mechanism is limited

Engineering Contradiction:
Improvesustained delivery durationVSAvoidredox-responsive release capability
Core Design Contradiction:
Duration of action of moving objectVSAdaptability or versatility

Solution Approach 1:

The patent applies parameter changes by utilizing the redox state of the environment as a trigger parameter for controlling drug release. The polydopamine nanoparticles are designed with redox-sensitive properties, meaning their structure and drug release characteristics change in response to variations in oxidative stress levels (ROS concentrations). When ROS levels increase, the nanoparticles undergo structural changes that accelerate therapeutic release. This parameter-based control mechanism allows the system to maintain sustained delivery over time while simultaneously adapting the release rate to the disease state, resolving the contradiction between extended duration and responsive capability.

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 compositions achieve a tailored release of therapeutics directly in response to pathophysiological indicators, enhancing treatment efficacy while minimizing side effects by targeting specific oxidative stress levels, thereby improving the management of ophthalmological disorders like age-related macular degeneration.

Implementation Method 1

redox-responsive release of therapeutics... increased release due to degradation upon exposure to ROS

Methodology Applied
Scientific EffectOxidation: Oxidation

Implementation Method 2

subsequent diffusion of surface-bound therapeutic... simple diffusion of therapeutic bound to the interior of the particles

Methodology Applied
Scientific EffectDiffusion: Diffusion

Data Source

PatentUS20230302156A1Redox-responsive nanoparticle compositions for ocular delivery of therapeutics
Publication Date: 2023.09.28 OHIO STATE INNOVATION FOUND
  • US20230302156A1 patent drawing
  • US20230302156A1 patent drawing
  • US20230302156A1 patent drawing

AI summary

The present disclosure relates to therapeutic compositions, and more particularly to redox-responsive nanoparticles that allow controlled release of therapeutics, such as vascular endothelial growth factor inhibitors, in body tissues such as in the eye.