Flavonoid-Polymer Nanocomplexes for Anti-Angiogenic Eye Therapy

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Solution Overview

Problem

Current treatments for age-related macular degeneration (AMD) caused by angiogenesis, such as intravitreal injections of anti-VEGF drugs, are associated with significant side effects, high costs, and the need for frequent injections, which pose challenges for patient compliance and medical burden.

Innovation Solution

A self-assembled nanocomplex comprising an active agent physically bound to a flavonoid-polymer conjugate, encapsulated by a second water-soluble polymer, which enhances drug delivery and stability, allowing for topical or intravitreal administration with reduced dosing frequency and improved bioavailability.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If intravitreal injections of anti-VEGF drugs are used to treat AMD, then visual acuity is improved, but side effects such as intraocular inflammation and increased intraocular pressure occur

Engineering Contradiction:
Improvevisual acuity improvementVSAvoidintraocular inflammation and increased intraocular pressure
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent uses flavonoid-polymer conjugates as intermediary carriers to deliver anti-VEGF drugs. The conjugates act as mediators between the drug and the target tissue, enabling controlled release and reducing direct tissue damage. The flavonoid-polymer conjugate system serves as a protective intermediary that maintains drug efficacy while minimizing harmful side effects at the injection site and within the eye.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent modifies the physical and chemical parameters of the drug delivery system by creating self-assembled nanocomplexes with specific size, charge, and surface properties. The nanocomplexes have controlled hydrodynamic diameter, zeta potential, and surface hydrophobicity to optimize their interaction with ocular tissues. These parameter changes enable the drug system to achieve therapeutic efficacy while reducing toxicity through optimized physical characteristics.

Inventive Principle:
Principle #35Parameter changes

2Reliability

If frequent intravitreal injections are administered to maintain treatment efficacy, then disease progression is controlled, but treatment cost and patient burden increase

Engineering Contradiction:
Improvedisease controlVSAvoidinjection frequency and treatment duration
Core Design Contradiction:
ReliabilityVSLoss of time

Solution Approach 1:

The patent implements sustained-release drug delivery systems using flavonoid-polymer conjugates that continuously release anti-VEGF drug over extended periods. The conjugates maintain therapeutic drug levels in the eye for months, providing continuous disease control without requiring frequent injections. This continuity of useful action reduces the frequency of medical interventions while maintaining treatment efficacy.

Inventive Principle:
Principle #20Continuity of useful action

Solution Approach 2:

The patent employs preliminary formulation of drugs into flavonoid-polymer conjugates with controlled release characteristics. The conjugates are pre-designed to release drug in a controlled manner over time, anticipating the need for sustained therapy. This preliminary action of creating sustained-release formulations allows for reduced injection frequency and long-term disease control without requiring continuous frequent interventions.

Inventive Principle:
Principle #10Preliminary action

3Reliability

If intravitreal injections are used to deliver anti-VEGF drugs, then treatment efficacy is achieved, but the invasive route causes tissue damage and infection risk

Engineering Contradiction:
Improvetreatment efficacyVSAvoidtissue damage and infection risk
Core Design Contradiction:
ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The patent uses flavonoid-polymer conjugates as intermediary carriers that facilitate drug delivery through alternative, less invasive routes. The conjugates act as mediators that can transport anti-VEGF drugs through the blood-ocular barrier or via topical application, avoiding the need for direct intravitreal needle insertion. This intermediary system maintains treatment efficacy while eliminating the invasive route and its associated tissue damage and infection risks.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent replaces the mechanical intravitreal injection system with alternative delivery mechanisms based on the flavonoid-polymer conjugate system. Instead of using mechanical needles and syringes to inject drugs directly into the vitreous, the system uses molecular-level interactions and controlled release mechanisms. This substitution of mechanical delivery with biochemical delivery systems eliminates physical trauma and infection risk while maintaining therapeutic efficacy.

Inventive Principle:
Principle #28Mechanics substitution (Replace mechanical system)

4Reliability

If conventional drug delivery systems are used for AMD treatment, then anti-angiogenic activity is achieved, but bioavailability and drug accumulation in the retina are insufficient

Engineering Contradiction:
Improveanti-angiogenic activityVSAvoiddrug accumulation in the retina
Core Design Contradiction:
ReliabilityVSQuantity of substance

Solution Approach 1:

The patent employs flavonoid-polymer conjugates as intermediary carriers that enhance drug transport to the retina. The conjugates act as mediators that facilitate blood-brain barrier penetration and ocular tissue accumulation. They improve the bioavailability of anti-VEGF drugs by enabling their passage through protective barriers and enhancing their accumulation in the target retina, thereby increasing anti-angiogenic activity without requiring higher drug doses.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent creates composite nanocomplex systems combining flavonoid-polymer conjugates with anti-VEGF drugs. This composite material approach leverages the beneficial properties of both components: the flavonoid-polymer conjugate provides enhanced bioavailability and tissue accumulation, while the anti-VEGF drug delivers therapeutic anti-angiogenic activity. The composite structure synergistically improves both drug delivery and therapeutic efficacy, achieving superior anti-angiogenic activity with optimized drug accumulation in the retina.

Inventive Principle:
Principle #40Composite materials

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 nanocomplex achieves enhanced and sustained anti-angiogenic activity with increased drug accumulation in the retina, reducing retinal lesion development and potentially prolonging treatment efficacy while minimizing side effects and injection frequency.

Implementation Method 1

a self-assembled nanocomplex comprising an active agent physically bound to a flavonoid-polymer conjugate

Methodology Applied
Scientific EffectSelf-assembly: Self-Assembly

Implementation Method 2

the nanocomplex is at least partially encapsulated by a second water-soluble polymer

Methodology Applied
Scientific EffectEncapsulation: Physical Containment

Implementation Method 3

increased drug accumulation in the retina

Methodology Applied
Scientific EffectAccumulation:

Data Source

PatentUS20240390503A1Green Tea-based Nanocomplexes for Eye Disease
Publication Date: 2024.11.28 SINGAPORE HEALTH SERVICES PTE LTD
  • US20240390503A1 patent drawing
  • US20240390503A1 patent drawing
  • US20240390503A1 patent drawing

AI summary

The present invention relates to a composition comprising a self-assembled nanocomplex, wherein the self-assembled nanocomplex comprises one or more active agent physically bound to one or more conjugate, wherein each conjugate comprises one or more flavonoid molecule and a first water-soluble polymer, and the nanocomplex is at least partially encapsulated by a second water-soluble polymer. The present invention also relates to a method of preparing the composition and uses thereof. The present invention also relates to a method of treating an eye disease caused by angiogenesis, comprising administering a composition to a subject in need thereof, wherein the composition comprises a self-assembled nanocomplex, wherein the self-assembled nanocomplex comprises an ophthalmic anti-angiogenesis drug physically bound to one or more conjugate, each conjugate comprising one or more flavonoid molecule and a first water-soluble polymer.