SP-Modified Liposome Delivery System for Blood-Brain Barrier Crossing

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Solution Overview

Problem

Current drug delivery systems face challenges in crossing the blood-brain barrier due to poor targeting efficiency caused by interactions with plasma proteins, leading to ineffective treatment of central nervous system diseases such as brain tumors.

Innovation Solution

A polypeptide modified delivery system utilizing amyloid β short peptide (SP) that specifically adsorbs apolipoproteins in plasma, forming a complex to cross the blood-brain barrier and target vascular endothelial cells and tumor cells, thereby enhancing the delivery of drugs and diagnostic molecules.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If traditional drug delivery systems are used to cross the blood-brain barrier, then the system structure is simple, but the targeting efficiency is poor due to interactions with plasma proteins

Engineering Contradiction:

Improvetargeting efficiencyVSAvoiddelivery system structure

Core Design Contradiction:

ReliabilityVSDevice complexity

Solution Approach 1:

The patent introduces amyloid β short peptide (SP) as an intermediary component that specifically binds to apolipoproteins in plasma. This intermediary mediates the interaction between the delivery system and plasma proteins, enabling the system to exploit the protein corona effect rather than suffer from it, thereby improving blood-brain barrier crossing efficiency and targeting to brain tumors

Inventive Principle:

Principle #24Intermediary (Mediator)

Solution Approach 2:

The delivery system is constructed as a composite structure combining SP-modified nanoparticles with therapeutic drugs. The composite material integrates the targeting functionality of SP-apolipoprotein complexes with the therapeutic payload, creating a multifunctional system that achieves both plasma protein regulation and effective brain tumor targeting

Inventive Principle:

Principle #40Composite materials

2Duration of action of moving object

If the delivery system interacts with plasma proteins to form protein corona, then the in vivo circulation is extended, but the targeting precision to brain tumors is reduced

Engineering Contradiction:

Improvein vivo circulation timeVSAvoidtargeting precision

Core Design Contradiction:

Duration of action of moving objectVSManufacturing precision

Solution Approach 1:

The patent converts the harmful effect of non-specific plasma protein adsorption into a beneficial targeting mechanism. By designing SP-modified nanoparticles, the system intentionally forms a protein corona enriched with apolipoproteins that specifically recognize brain tumor receptors, transforming the previously harmful protein corona effect into a precise targeting mechanism that simultaneously extends circulation and improves targeting precision

Inventive Principle:

Principle #22Blessing in disguise (Convert harm into benefit)

3Productivity

If receptor-mediated transport is used to cross the blood-brain barrier, then the drug delivery efficiency is improved, but the influence of body fluid components is ignored leading to poor in vivo performance

Engineering Contradiction:

Improvedrug delivery efficiencyVSAvoidin vivo performance

Core Design Contradiction:

ProductivityVSReliability

Solution Approach 1:

The patent applies preliminary action by pre-modifying the nanoparticle surface with amyloid β short peptide before administration. This pre-preparation ensures that the nanoparticles are equipped with the necessary targeting ligands to interact with plasma apolipoproteins and cross the blood-brain barrier efficiently, accounting for in vivo conditions beforehand and improving both delivery efficiency and in vivo performance

Inventive Principle:

Principle #10Preliminary action

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 SP-modified delivery system effectively crosses the blood-brain barrier, achieving targeted diagnosis and treatment of brain tumors and other brain diseases by regulating the protein corona and maintaining biological activity during circulation, improving therapeutic outcomes.

Implementation Method 1

specifically adsorb apolipoprotein in plasma

Methodology Applied

Scientific EffectAdsorption: Adsorption

Data Source

PatentUS12178885B2Method for mediating targeted delivery of a composition to the brain of a subject in need thereof

Publication Date: 2024.12.31 FUDAN UNIVERSITY

AI summary

A polypeptide modified complex in the pharmaceutical field that can specifically adsorb apolipoproteins in plasma and can mediate a drug across the blood-brain barrier, a target delivery system, and use thereof in preparation of a formulation for diagnosing and treating brain tumors and other brain diseases. The polypeptide fragment (SP) of the amyloid β (relating to one type) is modified shown that the modified delivery system increases uptake the of the amyloid β by vascular endothelial cells after the modified delivery system forms a protein crown with plasma proteins. The modified liposome delivery system delivers a drug to the lesion site more effectively, significantly improving the therapeutic effect of the drug. After the SP adsorbs plasma proteins, a drug may be mediated across the blood-brain barrier and/or targeted to tumor neovascular and tumor cells, and the modified drug and delivery system thereof obtain a better therapeutic effect when treating brain tumors and other diseases in the brain.