Blood-Brain Barrier Peptides for Hydrophilic Drug Delivery

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Solution Overview

Problem

The blood-brain barrier's selective permeability hinders the delivery of hydrophilic therapeutic agents for treating brain and central nervous system diseases such as Alzheimer's and Parkinson's, as they cannot pass through the barrier.

Innovation Solution

Development of blood-brain barrier permeable peptides, specifically with amino acid sequences SEQ ID NO: 3 or SEQ ID NO: 5, which can be fused with cell membrane permeable peptides like Penetratin or GST, allowing for the delivery of target materials across the barrier.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If hydrophilic therapeutic agents are used to treat brain and CNS diseases, then treatment effectiveness is improved, but the agents cannot pass through the blood-brain barrier

Engineering Contradiction:
Improvetreatment effectivenessVSAvoidbarrier permeability limitation
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent uses permeability peptides as intermediary carriers that can transport hydrophilic therapeutic agents across the blood-brain barrier. These peptides act as mediators between the therapeutic agent and the barrier, enabling delivery that would otherwise be impossible. The peptides bind to the therapeutic agents and facilitate their passage through the barrier via cellular uptake mechanisms.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The invention creates composite delivery systems by combining permeability peptides with therapeutic agents. This composite approach allows the therapeutic agent to gain the permeability properties of the peptide carrier, enabling hydrophilic drugs to cross the blood-brain barrier while maintaining their therapeutic activity.

Inventive Principle:
Principle #40Composite materials

2Object-affected harmful factors

If the blood-brain barrier maintains high selective permeability, then protection from pathogens and toxins is improved, but delivery of therapeutic agents is hindered

Engineering Contradiction:
Improveprotection from pathogensVSAvoiddrug delivery capability
Core Design Contradiction:
Object-affected harmful factorsVSEase of manufacture

Solution Approach 1:

Permeability peptides serve as intermediary carriers that exploit the barrier's existing transport mechanisms. Rather than overcoming the barrier's protective function, the peptides utilize its cellular uptake pathways to deliver therapeutic agents, thereby maintaining protection while enabling delivery.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent modifies the delivery approach by changing the parameters of the therapeutic agent delivery system. By attaching permeability peptides to therapeutic agents, the system changes its physical and chemical properties to match the permeability characteristics required for barrier passage, while the barrier's selective permeability remains intact for its protective function.

Inventive Principle:
Principle #35Parameter changes

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 peptides effectively deliver therapeutic agents and diagnostic agents to the brain, enabling treatment and diagnosis of neurological diseases by overcoming the barrier's permeability limitations.

Implementation Method 1

The blood-brain barrier plays a role of passively allowing glucose, essential amino acids, electrolytes and the like to pass through it through endothelial cells

Methodology Applied
Scientific EffectPassive transport: Diffusion

Implementation Method 2

fusion proteins of 5 kinds of novel peptides and GST passed through the blood-brain barrier through in vivo experimental results

Methodology Applied
Scientific EffectCellular permeation: Permeation

Data Source

PatentUS20250367303A1Polypeptide that passes through blood-brain barrier, and use thereof
Publication Date: 2025.12.04 MEDI&GENE
  • US20250367303A1 patent drawing
  • US20250367303A1 patent drawing
  • US20250367303A1 patent drawing

AI summary

The present invention relates to a polypeptide that passes through a blood-brain barrier or cerebrovascular barrier and a use of the polypeptide for material delivery, and the polypeptide can deliver a material that naturally cannot pass through the blood-brain barrier such as protein into brain tissue.