Sustained-Release Antioxidant Formulations for Ocular and Tumor Therapy

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Solution Overview

Problem

Current treatments for ocular afflictions and cancers using oral antioxidants have shown moderate to poor results due to challenges in maintaining therapeutic levels, with high oral doses of antioxidants like vitamin C being ineffective, highlighting the need for minimally invasive injectable or implantable sustained release formulations to target reactive oxygen species effectively.

Innovation Solution

Development of novel liquid and solid, sustained release formulations of biocompatible, biodegradable excipients containing antioxidants for intraocular or intratumoral injection or implantation, which maintain therapeutic levels of antioxidants at the site of treatment, using combinations such as tocopheryl esters with ascorbic acid and glutathione, and other antioxidants like resveratrol and timolol, to scavenge reactive oxygen species.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of operation

If oral administration of antioxidants is used, then the treatment is simple and non-invasive, but the therapeutic levels of antioxidants cannot be maintained in the target tissue

Engineering Contradiction:

ImproveEase of administrationVSAvoidTherapeutic level maintenance

Core Design Contradiction:

Ease of operationVSReliability

Solution Approach 1:

The patent uses biocompatible, biodegradable excipients as intermediary carriers to deliver antioxidants directly to the target tissue. These excipients serve as a mediator between the antioxidant and the target site, enabling sustained release and maintaining therapeutic levels without requiring continuous oral administration.

Inventive Principle:

Principle #24Intermediary (Mediator)

Solution Approach 2:

The invention segments the antioxidant delivery system into controlled-release formulations that release the antioxidant gradually over time. This segmentation of the delivery mechanism allows maintenance of therapeutic levels through sustained release rather than frequent dosing.

Inventive Principle:

Principle #1Segmentation

2Quantity of substance

If high oral doses of antioxidants are administered, then the dosage is sufficient to potentially achieve therapeutic effects, but the antioxidants still cannot reach effective concentrations in the target tissue

Engineering Contradiction:

ImproveAntioxidant dosageVSAvoidTherapeutic concentration achievement

Core Design Contradiction:

Quantity of substanceVSReliability

Solution Approach 1:

The patent applies local quality by concentrating the antioxidant delivery directly at the target tissue site rather than relying on systemic distribution. The excipients are designed to localize the antioxidant release specifically in the target tissue, ensuring high local concentrations where needed.

Inventive Principle:

Principle #3Local quality

Solution Approach 2:

The biocompatible excipients act as intermediaries that facilitate the transport and localization of antioxidants to the target tissue, enabling the quantity of substance to be effectively delivered to the right location rather than being distributed systemically where it cannot achieve sufficient concentration.

Inventive Principle:

Principle #24Intermediary (Mediator)

3Reliability

If sustained release formulations are developed for injectable or implantable delivery, then therapeutic levels of antioxidants can be maintained at the treatment site, but the device complexity and administration invasiveness increase

Engineering Contradiction:

ImproveTherapeutic level maintenanceVSAvoidFormulation complexity

Core Design Contradiction:

ReliabilityVSDevice complexity

Solution Approach 1:

The patent changes the physical and chemical parameters of the antioxidant formulation by incorporating biocompatible, biodegradable excipients. These parameter changes enable sustained release properties while maintaining biocompatibility, achieving reliable therapeutic level maintenance without excessive complexity.

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The invention uses composite materials combining antioxidants with biocompatible, biodegradable excipients. This composite approach enables sustained release functionality while the biodegradable nature of the excipients simplifies the overall system by eliminating the need for retrieval or long-term presence of the delivery vehicle.

Inventive Principle:

Principle #40Composite materials

4Reliability

Engineering Contradiction:

ImproveTherapeutic level maintenanceVSAvoidAdministration invasiveness

Core Design Contradiction:

ReliabilityVSEase of operation

Solution Approach 1:

The patent employs biodegradable excipients that are designed to be temporary and self-dissipating. These short-living delivery vehicles perform their function of maintaining therapeutic levels and then naturally degrade, eliminating the need for complex retrieval procedures and reducing the invasiveness of the overall treatment approach.

Inventive Principle:

Principle #27Cheap short-living objects (Disposable)

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

These formulations provide effective and sustained delivery of antioxidants, maintaining therapeutic levels for extended periods, effectively treating ocular disorders and tumors by scavenging reactive oxygen species, with the potential to enhance existing therapies and provide synergistic benefits when combined with other treatments.

Implementation Method 1

sustained release formulations of biocompatible, biodegradable excipients containing antioxidants for intraocular or intratumoral injection or implantation

Methodology Applied

Scientific EffectSustained release: