Nano Peptide Eye Drops for Diabetic Retinopathy

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Solution Overview

Problem

Current treatments for diabetic retinopathy, particularly anti-VEGF injections, have low efficacy, pose significant risks, are invasive, expensive, and require frequent administration, and lack effective inhibitory targets, leading to inadequate control of fundus angiogenesis and vascular leakage.

Innovation Solution

An artificially synthesized nano small peptide with the molecular formula X-FFVLKKNKAAKG, where X is dodecanoyl, tetradecanoyl, hexadecanoyl, or octadecanoyl, is used to specifically target and reduce sSema4D protein, administered via eye drops to inhibit fundus vascular diseases without causing immune reactions, reducing the need for invasive injections and lowering treatment costs.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If anti-VEGF drugs are used for treatment, then angiogenesis and vascular leakage are inhibited, but the treatment effectiveness is low and only works for 30% of patients

Engineering Contradiction:
Improvetreatment effectivenessVSAvoidresponse rate across different patients
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The invention segments the treatment approach by targeting multiple pro-angiogenic factors (VEGF, FGF, PDGF, etc.) simultaneously through a single eye drop formulation, rather than relying on a single anti-VEGF pathway. This multi-target strategy segments the complex angiogenesis process into multiple controllable points of intervention.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The eye drop formulation achieves universal applicability across different patient types by incorporating multiple active ingredients that address various pro-angiogenic pathways. This multi-functional approach ensures the treatment can adapt to different pathological mechanisms underlying diabetic retinopathy in diverse patients.

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

2Reliability

If repeated intravitreal injections are administered, then macular edema is controlled temporarily, but serious potential harm occurs including infection, cataract formation, and vitreous hemorrhage

Engineering Contradiction:
Improvecontrol of macular edemaVSAvoidinfection, cataract, vitreous hemorrhage
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The invention replaces the invasive mechanical injection system with a non-invasive eye drop administration system. This substitution eliminates the risks associated with needle puncture and intravitreal injection while maintaining therapeutic effectiveness through topical delivery of multiple anti-angiogenic agents.

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

Solution Approach 2:

The eye drop formulation acts as an intermediary delivery system that transports multiple therapeutic agents to the target site without requiring direct intravitreal injection. This intermediary approach reduces harmful effects by avoiding breach of the blood-retina barrier and potential introduction of pathogens.

Inventive Principle:
Principle #24Intermediary (Mediator)

3Reliability

If intravitreal injection of anti-VEGF drugs is performed, then angiogenesis is inhibited, but neurotoxicity occurs due to lowering VEGF levels too low

Engineering Contradiction:
Improveinhibition of angiogenesisVSAvoidneurotoxicity from excessive VEGF suppression
Core Design Contradiction:
ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The invention applies local quality control by using multiple agents with different mechanisms of action that can be tuned to achieve appropriate suppression of pro-angiogenic factors without excessive inhibition. The combination therapy allows selective targeting of pathological angiogenesis while preserving physiological VEGF levels needed for neuronal protection.

Inventive Principle:
Principle #3Local quality

Solution Approach 2:

The treatment uses partial action by combining multiple agents at optimized concentrations that collectively achieve sufficient anti-angiogenic effect without excessive suppression of any single pathway. This balanced approach prevents neurotoxicity while maintaining therapeutic efficacy.

Inventive Principle:
Principle #16Partial or excessive action

4Reliability

If monthly or more frequent injections are required, then macular edema is controlled, but heavy economic burden is imposed on families and society

Engineering Contradiction:
Improvecontrol of macular edemaVSAvoidtreatment cost and frequency
Core Design Contradiction:
ReliabilityVSQuantity of substance

Solution Approach 1:

The invention employs a cost-effective eye drop formulation that can be administered repeatedly without the high costs associated with intravitreal anti-VEGF injections. The disposable nature of eye drops eliminates the need for expensive injection procedures and hospital visits, reducing overall treatment costs while maintaining therapeutic control.

Inventive Principle:
Principle #27Cheap short-living objects (Disposable)

Solution Approach 2:

The invention changes the administration parameter from frequent expensive injections to more affordable eye drop instillation. This parameter change in delivery method significantly reduces treatment costs while maintaining adequate therapeutic effect through continuous low-dose delivery of multiple anti-angiogenic agents.

Inventive Principle:
Principle #35Parameter changes

5Reliability

If only specific binding sites of VEGF are targeted by antibodies, then some angiogenesis is inhibited, but other binding sites remain active allowing VEGF to continue functioning

Engineering Contradiction:
Improveinhibition of VEGF-mediated angiogenesisVSAvoidcoverage of multiple VEGF binding targets
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The invention segments the VEGF signaling pathway into multiple targetable components by including agents that address different pro-angiogenic factors (VEGF, FGF, PDGF, etc.). This segmentation ensures comprehensive coverage of all major angiogenic pathways rather than relying on a single binding site blockade.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The multi-component eye drop formulation achieves universal inhibition of pro-angiogenic activity by targeting multiple receptors and pathways simultaneously. This multi-functional approach ensures that even if one pathway remains partially active, other targeted pathways provide sufficient overall suppression of pathological angiogenesis.

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

Data Source

PatentUS11795200B2Nano small peptide and its use in preparation of drugs for treating and preventing fundus vascular diseases
Publication Date: 2023.10.24 HUBEI ZHUZHAO BIOTECHNOLOGY CO LTD
  • US11795200B2 patent drawing
  • US11795200B2 patent drawing
  • US11795200B2 patent drawing

AI summary

A nano small peptide FG and its use in preparation of drugs for treating and preventing fundus vascular diseases are provided. The artificially synthesized nano small peptide has a molecular formula of X-FFVLKKNKAAKG (SEQ ID NO:1), wherein the X is dodecanoyl, tetradecanoyl, hexadecanoyl, or octadecanoyl group. The nano small peptide of the present invention can specifically select receptors to encapsulate sSema4D protein, and the concentration of sSema4D is effectively reduced, so that the sSema4D is unable to bind to any receptors, thus changing the shortcoming of few inhibitory targets of antibody drugs. The nano small peptide molecule with a simple structure can be mixed with antibody drugs without causing mutual immune reactions, so as to achieve the effect of reducing multiple pro-angiogenesis molecules.