Fusion Peptide Derivative for Brain Barrier Delivery

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Solution Overview

Problem

Peptides administered intranasally face challenges in crossing the blood-brain barrier and are prone to enzymatic decomposition, limiting their effectiveness and duration of action.

Innovation Solution

A centrally-acting peptide derivative is developed by combining a centrally-acting peptide sequence with a cell-penetrating sequence and an endosomal-escape sequence, enhancing its ability to migrate to the central nervous system and resist enzymatic degradation.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of operation

If a peptide is administered intranasally, then the administration is less invasive and can deliver peptide to the central nervous system, but the peptide does not easily pass the blood-brain barrier and the effect is lost within a short period due to enzymatic decomposition

Engineering Contradiction:
Improveadministration invasivenessVSAvoidpeptide stability and brain delivery efficiency
Core Design Contradiction:
Ease of operationVSReliability

Solution Approach 1:

The patent applies composite materials by fusing the centrally-acting peptide with a cell-penetrating peptide sequence to create a hybrid peptide derivative. This composite structure combines the pharmacological activity of the centrally-acting peptide with the blood-brain barrier crossing capability of the cell-penetrating peptide, enabling efficient brain delivery while maintaining the therapeutic effect

Inventive Principle:
Principle #40Composite materials

Solution Approach 2:

The cell-penetrating peptide sequence acts as an intermediary that facilitates the transport of the centrally-acting peptide across the blood-brain barrier. This intermediary component enables the peptide to traverse the barrier without direct interaction between the centrally-acting peptide and the barrier, solving the delivery efficiency problem

Inventive Principle:
Principle #24Intermediary (Mediator)

2Ease of operation

If a peptide is administered intranasally, then the administration is less invasive, but the peptide is prone to enzymatic decomposition in a biological body

Engineering Contradiction:
Improveadministration invasivenessVSAvoidpeptide stability
Core Design Contradiction:
Ease of operationVSStability of the object's composition

Solution Approach 1:

The patent uses composite materials by creating a fusion peptide that combines the centrally-acting peptide with a cell-penetrating peptide sequence. This composite structure provides enhanced stability by protecting the centrally-acting peptide from enzymatic decomposition while maintaining its pharmacological activity

Inventive Principle:
Principle #40Composite materials

Solution Approach 2:

The cell-penetrating peptide sequence serves as a protective layer that shields the centrally-acting peptide from enzymatic degradation in the biological body. This beforehand cushioning effect prevents the peptide from being decomposed before it can reach its target in the central nervous system

Inventive Principle:
Principle #11Beforehand cushioning (Prior cushioning)

Data Source

PatentEP3190129B1Centrally-acting peptide derivative, and pharmaceutical composition
Publication Date: 2020.01.08 TOKYO UNIVERSITY OF SCIENCE
  • EP3190129B1 patent drawingFigure 1
  • EP3190129B1 patent drawingFigure 2
  • EP3190129B1 patent drawingFigure 3

AI summary

A centrally-acting peptide derivative, including a centrally-acting portion, a cell-penetrating sequence portion, and an endosomal-escape portion.