SC79 Blood-Brain Barrier Permeability Regulation for Brain Drug Delivery

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Solution Overview

Problem

The blood-brain barrier (BBB) limits the transportation of therapeutic drugs into the brain, reducing the efficacy of drug therapy for brain diseases, and existing brain targeting drug delivery systems fail to account for changes in BBB permeability during disease treatment.

Innovation Solution

A blood-brain barrier permeability regulator comprising SC79 or its analogue, which down-regulates tight junction proteins Claudin-5 and Occludin by activating the Claudin-5 and Occludin signaling pathway downstream protein kinase B, enhancing the efficiency of an Angiopep-2-modified glycolipid nano-delivery system to transport drugs into the brain.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If the blood-brain barrier maintains its integrity to protect the central nervous system, then the protective function is improved, but the transportation of therapeutic drugs into the brain deteriorates

Engineering Contradiction:

Improveprotective function of blood-brain barrierVSAvoidtransportation efficiency of therapeutic drugs

Core Design Contradiction:

ReliabilityVSProductivity

Solution Approach 1:

The patent applies preliminary action by using SC79 to temporarily increase BBB permeability before administering the brain-targeting drug delivery system. This preliminary modification of BBB permeability creates a favorable condition for subsequent drug transport, allowing the therapeutic system to enter the brain more efficiently while the BBB subsequently returns to its normal protective state

Inventive Principle:

Principle #10Preliminary action

Solution Approach 2:

The patent employs dynamics by making the BBB permeability adjustable rather than static. Through the use of SC79, the BBB permeability can be dynamically modified to increase during drug delivery and then return to baseline, allowing the system to adapt between protective function and drug transport requirements

Inventive Principle:

Principle #15Dynamics

2Productivity

If the blood-brain barrier permeability increases due to pathological destruction, then the transportation of drug delivery system into the brain is enhanced, but the environmental balance of the central nervous system deteriorates

Engineering Contradiction:

Improvetransportation efficiency of drug delivery systemVSAvoidenvironmental unbalance in central nervous system

Core Design Contradiction:

ProductivityVSObject-affected harmful factors

Solution Approach 1:

The patent uses SC79 as an intermediary substance that temporarily and controllably increases BBB permeability. Unlike pathological destruction which causes uncontrolled permeability increase, SC79 acts as a mediator that produces a controlled, reversible effect, allowing enhanced drug transport without the harmful environmental unbalance caused by disease

Inventive Principle:

Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent applies parameter changes by temporarily modifying the permeability parameter of the BBB through SC79 treatment. This controlled parameter change enables enhanced drug delivery while avoiding the uncontrolled pathological changes that lead to environmental unbalance in the CNS

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

The regulator increases BBB permeability, improving the efficiency and efficacy of brain targeting drug delivery systems, particularly for glioma treatment, by maintaining BBB function during therapy.

Implementation Method 1

SC79 or an analogue thereof, which down-regulates tight junction proteins Claudin-5 and Occludin by activating the Claudin-5 and Occludin signaling pathway downstream protein kinase B

Methodology Applied

Scientific EffectProtein kinase B signaling pathway activation:

Implementation Method 2

receptor-mediated trans-endocytosis is considered as one of the most effective pathways for brain targeting delivery due to its high affinity, selectivity and specificity

Methodology Applied

Scientific EffectReceptor-mediated trans-endocytosis:

Implementation Method 3

Angiopep-2 is an aprotinin-derived polypeptide that targets specifically the low density lipoprotein receptor-associated protein 1. The low density lipoprotein receptor-associated protein 1 is highly expressed in both the blood-brain barrier and the glioma cell

Methodology Applied

Scientific EffectReceptor-ligand binding:

Data Source

PatentUS12370167B2Blood-brain barrier permeability regulator and use thereof

Publication Date: 2025.07.29 ZHEJIANG UNIV

AI summary

The present invention relates to use of SC79 or an analogue thereof in the preparation of a blood-brain barrier permeability regulator. The blood-brain barrier permeability regulator comprises SC79 or an analogue thereof as an active ingredient, which down-regulates expression of tight junction proteins Claudin-5 and Occludin by activating Claudin-5 and Occludin signaling pathway downstream the protein kinase B, and thereby increases the blood-brain barrier permeability, and enhances the efficiency of transportation of a brain targeting drug delivery system, especially, an Angiopep-2-modified glycolipid nano-delivery system, into the brain. The present invention also relates to a kit comprising the blood-brain barrier permeability regulator and a brain targeting drug delivery system. According to the present invention, use of the blood-brain barrier permeability regulator in combination with a brain targeting drug delivery system can enhance the efficiency of transportation of a brain targeting drug delivery system into the brain, and thereby improve the therapeutic efficacy of the brain targeting drug delivery system.