Collagen Type I Carrier for Sustained PEDF Peptide Release

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Solution Overview

Problem

Current treatments for age-related macular degeneration, particularly exudative type, face challenges due to the short half-life and narrow concentration range of pigment epithelium-derived factor (PEDF), requiring frequent injections and limited therapeutic efficacy.

Innovation Solution

A pharmaceutical composition combining collagen type I with a 34-mer PEDF peptide, which acts as a carrier to maintain intraocular antiangiogenic effects, extending the antiangiogenic activity cycle and reducing the frequency of injections.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If PEDF is used as a therapeutic agent for macular degeneration, then antiangiogenic effect is achieved, but treatment requires frequent injections due to short half-life

Engineering Contradiction:
Improvetherapeutic efficacyVSAvoidtreatment frequency
Core Design Contradiction:
ReliabilityVSLoss of time

Solution Approach 1:

The patent uses collagen type I as an intermediary carrier to deliver PEDF peptide to the target site. The collagen matrix serves as a sustained-release system that maintains PEDF at effective concentrations over extended periods, eliminating the need for frequent injections while maintaining reliable therapeutic efficacy against neovascularization in macular degeneration

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent changes the concentration parameter of PEDF from high-dose intermittent administration to low-dose continuous administration through collagen-mediated sustained release. This parameter transformation maintains antiangiogenic efficacy while extending the effective treatment window and reducing injection frequency

Inventive Principle:
Principle #35Parameter changes

2Reliability

If high dose of PEDF is administered, then antiangiogenic effect is enhanced, but angiogenic effect occurs due to narrow concentration range

Engineering Contradiction:
Improveantiangiogenic effectVSAvoidangiogenic effect
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

Collagen type I acts as a mediator that controls the release kinetics of PEDF, ensuring concentrations remain within the therapeutic window. The collagen matrix prevents both under-dosing (ineffective) and over-dosing (angiogenic), maintaining PEDF levels that consistently inhibit neovascularization without triggering harmful angiogenic responses

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The collagen carrier provides periodic, controlled release of PEDF peptide, creating sustained oscillating concentrations that maintain antiangiogenic pressure. This periodic delivery pattern prevents the concentration spikes that would trigger angiogenic effects while avoiding the troughs that would reduce therapeutic efficacy

Inventive Principle:
Principle #19Periodic action

Data Source

PatentEP3636275B1Pharmaceutical composition for preventing or treating neovascular disease, containing collagen type i and pigment epithelium derived factor peptide as active ingredients
Publication Date: 2023.08.09 NEXTHERA CO LTD
  • EP3636275B1 patent drawingFigure 1A~1D
  • EP3636275B1 patent drawingFigure 2A~3B
  • EP3636275B1 patent drawingFigure 4A~4B

AI summary

The present invention relates to a pharmaceutical composition for preventing or treating neovascular disease, comprising a collagen and a 34-mer pigment epithelium derived factor (PEDF) peptide as an active ingredient, more specifically, the combined administration of the collagen type I and the 34-mer pigment epithelium derived factor peptide increases the short antiangiogenic activity cycle of the PEDF and extends the dosage range of the PEDF to solve the discomfort and the side effects accordingly due to the conventional frequent injections and thus it can be applied as a therapeutic agent for various neovascular diseases.