BBB-Targeting Liposomes for Selective Brain Drug Delivery

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Solution Overview

Problem

The blood-brain barrier (BBB) poses a significant obstacle to drug delivery to the brain, leading to non-selective permeability and interference with therapeutic efficacy, as existing strategies often disrupt the BBB's integrity and lack specificity.

Innovation Solution

A liposome-based composition conjugated with a short Apolipoprotein E or Amyloid beta recognition peptide, composed of cholesterol, 1,2-dioleoyl-sn-glycero-3-phosphocholine (DOPC), and 1,2-dioleoyl-sn-glycero-3-phosphoethanolamine (DOPE), targets the BBB for controlled and safe drug delivery without disrupting its integrity.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Productivity

If conventional strategies are used to enhance drug permeation through the BBB, then drug delivery capacity is improved, but BBB integrity is disrupted and selectivity is lost

Engineering Contradiction:
Improvedrug delivery capacityVSAvoidBBB integrity
Core Design Contradiction:
ProductivityVSReliability

Solution Approach 1:

The patent uses liposomes as intermediary carriers that can interact with BBB transport systems without disrupting the barrier. The liposomes are designed to be recognized by BBB transport mechanisms (such as LDL receptors or transferrin receptors), allowing them to cross the BBB through physiological pathways rather than forcing permeation that would damage the barrier.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent modifies the physical and chemical parameters of drug delivery by encapsulating drugs in liposomes with specific surface properties, sizes, and compositions. These parameter changes allow the delivery system to exploit BBB transport mechanisms while maintaining barrier integrity, rather than using high concentrations or harsh methods that would disrupt the BBB.

Inventive Principle:
Principle #35Parameter changes

2Productivity

If drugs are modified to enable BBB permeation, then delivery capability is improved, but therapeutic specificity is reduced

Engineering Contradiction:
ImproveBBB permeation capabilityVSAvoidtherapeutic specificity
Core Design Contradiction:
ProductivityVSMeasurement precision

Solution Approach 1:

The patent separates the drug from the BBB-crossing function by using liposomes as distinct carriers. The liposome surface is modified with ligands that recognize BBB transport systems, while the therapeutic drug remains encapsulated inside. This segmentation allows the crossing function and therapeutic function to be independently optimized, maintaining drug specificity while enabling BBB penetration.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The liposome acts as an intermediary that carries the drug across the BBB without requiring the drug itself to be modified. The liposome surface contains recognition elements that interact with BBB transport systems, while the enclosed drug maintains its original therapeutic properties and specificity.

Inventive Principle:
Principle #24Intermediary (Mediator)

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 composition enables effective and selective drug delivery across the BBB, minimizing side effects and maintaining BBB integrity, enhancing therapeutic efficacy and reducing off-target distribution.

Implementation Method 1

The BBB also contains a number of specific transport and enzyme systems that regulate molecular traffic across the blood capillaries. The latter includes carrier-mediated transport (CMT) for low molecular weight nutrient or receptor-mediated transport (RMT) for circulating peptides and plasma proteins.

Methodology Applied
Scientific EffectReceptor-mediated transport:

Implementation Method 2

The present invention provides a composition comprising a liposome and an anchored blood-brain-barrier (BBB) recognition peptide conjugated to said liposome

Methodology Applied
Scientific EffectLiposome-mediated delivery:

Implementation Method 3

a short Apolipoprotein E recognition peptide and/or a short Amyloid beta recognition peptide is/are conjugated to the liposome

Methodology Applied
Scientific EffectPeptide recognition and binding: Adsorption

Data Source

PatentEP2919760B1Liposomes with an anchored blood brain barrier recognition peptide for an improved delivery of a drug into the brain
Publication Date: 2026.03.18 TECHNION RES & DEV FOUND LTD
  • EP2919760B1 patent drawingFigure 1
  • EP2919760B1 patent drawingFigure 2A~2C1
  • EP2919760B1 patent drawingFigure 3A~3B

AI summary

The present invention provides a liposome based composition wherein the liposome includes a peptide conjugated thereto via a peptide bond, wherein the peptide includes a spacer amino acid and a short Apolipoprotein E recognition sequence or a short Amyloid beta recognition sequence. This invention further provides a process for making the liposome and methods of utilizing the liposome based composition for therapeutic and diagnostic purposes.