Redox-Responsive Disulfide Nanoparticles for Targeted Ocular Drug Delivery

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Solution Overview

Problem

There is a need for improved drug delivery systems that can effectively prevent vision loss by targeting oxidative stress-induced conditions in the eye, such as age-related macular degeneration and proliferative vitreoretinopathy, using redox-responsive disulfide nanoparticles to encapsulate tyrosine kinase inhibitors like dasatinib.

Innovation Solution

The development of redox-responsive disulfide nanoparticles, derived from phospholipid-PEG, encapsulating tyrosine kinase inhibitors, which release the drug in response to oxidative stress, providing targeted delivery to ocular tissues.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Measurement precision

If conventional drug delivery systems are used, then drug delivery is simple, but delivery precision and targeting capability are insufficient

Engineering Contradiction:

Improvedelivery precisionVSAvoidsystem complexity

Core Design Contradiction:

Measurement precisionVSDevice complexity

Solution Approach 1:

The drug delivery system is segmented into distinct functional components: redox-responsive disulfide nanoparticles as carriers, tyrosine kinase inhibitor as payload, and PEG coating for stabilization. This segmentation allows each component to be optimized independently while maintaining overall system precision for targeted ocular delivery

Inventive Principle:

Principle #1Segmentation

Solution Approach 2:

The redox-responsive disulfide nanoparticles act as an intermediary between the hydrophobic tyrosine kinase inhibitor and the aqueous ocular environment. The nanoparticles mediate drug solubilization, protection, and targeted delivery, bridging the gap between drug properties and delivery requirements

Inventive Principle:

Principle #24Intermediary (Mediator)

2Duration of action of moving object

If drug delivery is sustained over time, then therapeutic effect is improved, but drug release control becomes more difficult

Engineering Contradiction:

Improvesustained deliveryVSAvoidrelease control

Core Design Contradiction:

Duration of action of moving objectVSEase of operation

Solution Approach 1:

The nanoparticle system incorporates dynamic redox-responsive disulfide bonds that can reversibly change conformation and stability in response to cellular redox conditions. This dynamic property enables sustained drug delivery while maintaining responsive release control when encountering oxidative stress environments in diseased ocular tissues

Inventive Principle:

Principle #15Dynamics

Solution Approach 2:

The system exploits changes in redox potential as a controlling parameter for drug release. The disulfide bonds remain stable under normal physiological reducing conditions, providing sustained delivery, but undergo reduction to release the drug when exposed to elevated oxidative conditions in pathological ocular tissues

Inventive Principle:

Principle #35Parameter changes

3Reliability

If drug encapsulation efficiency is increased, then therapeutic effectiveness is improved, but manufacturing precision requirements increase

Engineering Contradiction:

Improvetherapeutic effectivenessVSAvoidencapsulation precision

Core Design Contradiction:

ReliabilityVSManufacturing precision

Solution Approach 1:

The nanoparticle formulation utilizes self-assembly of phospholipid-PEG conjugates with embedded disulfide bonds, which spontaneously encapsulate the hydrophobic tyrosine kinase inhibitor during formulation preparation. This self-service mechanism achieves high encapsulation efficiency without requiring complex manufacturing processes or precise control equipment

Inventive Principle:

Principle #25Self-service

4Reliability

If drug delivery is targeted to ocular tissues, then therapeutic effectiveness is improved, but system complexity increases

Engineering Contradiction:

Improvetargeted deliveryVSAvoiddelivery system complexity

Core Design Contradiction:

ReliabilityVSDevice complexity

Solution Approach 1:

The nanoparticle system exhibits local quality through its redox-responsive特性 that are specifically activated in the ocular tissue environment where oxidative stress is elevated. The disulfide bonds remain inert in circulation but become active upon reaching the target site, providing targeted delivery without requiring complex targeting moieties

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

The nanoparticles provide sustained and targeted delivery of tyrosine kinase inhibitors, effectively preventing or treating ocular injuries and diseases by reducing oxidative stress and associated conditions, with minimal toxicity.

Implementation Method 1

the pharmaceutical composition releases the tyrosine kinase inhibitor in response to a redox condition, for example when subjected to oxidative stress and/or in the presence of reactive oxygen species

Methodology Applied

Scientific EffectRedox reactions: Redox Reactions

Data Source

PatentUS20260014091A1Compositions and methods of making and use thereof

Publication Date: 2026.01.15 OHIO STATE INNOVATION FOUND

AI summary

Disclosed herein are compositions and methods of making and use thereof. For example, disclosed herein are pharmaceutical compositions comprising: a plurality of redox-responsive disulfide nanoparticles; and a tyrosine kinase inhibitor encapsulated within each of the redox-responsive disulfide nanoparticles. Also disclosed herein are methods of treating or preventing an ocular injury, disease, or disorder in a subject in need thereof, the methods comprising administering a therapeutically effective amount of a plurality of redox-responsive disulfide nanoparticles and/or any of the pharmaceutical compositions disclosed herein to the subject.