Borneol-Plant Protein Mixture Enhances Blood-Brain Barrier Permeability

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Solution Overview

Problem

Current drugs targeting the central nervous system (CNS) face challenges in permeating the blood-brain barrier (BBB), limiting their therapeutic efficacy for conditions like Alzheimer's disease, stroke cerebral ischemia, and cerebral edema due to the barrier's restrictive nature.

Innovation Solution

A process involving the combination of borneol with high purity plant proteins, resulting in a stable mixture (PB-154) that enhances BBB permeability, allowing for improved delivery of bioactive molecules to the brain, which is then formulated into dietary supplements.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If drugs are administered to treat CNS disorders, then therapeutic efficacy is intended, but the blood-brain barrier prevents permeation of drugs into the brain

Engineering Contradiction:
Improvetherapeutic efficacyVSAvoidblood-brain barrier obstruction
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent uses borneol as an intermediary substance to facilitate drug permeation across the blood-brain barrier. Borneol temporarily modifies the barrier properties, allowing therapeutic drugs to pass through, and then returns to its original state. This mediator approach resolves the contradiction by introducing a third substance that temporarily overcomes the barrier without permanently compromising its protective function.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent employs borneol to temporarily alter the physical-chemical parameters of the blood-brain barrier, specifically increasing its permeability to therapeutic molecules. This parameter change is transient and reversible, allowing drugs to pass through during the treatment window while maintaining barrier integrity afterward, thus resolving the contradiction between barrier protection and drug delivery.

Inventive Principle:
Principle #35Parameter changes

2Productivity

If borneol is used to increase BBB permeability, then drug delivery to brain is improved, but stability of borneol solution decreases

Engineering Contradiction:
Improvedrug delivery efficiencyVSAvoidborneol solution stability
Core Design Contradiction:
ProductivityVSStability of the object's composition

Solution Approach 1:

The patent creates a composite system by combining borneol with plant proteins (such as soy protein, rice protein, or wheat protein) to form a stable conjugate. This composite material approach allows the borneol to maintain its BBB-opening functionality while the plant protein matrix provides structural stability and prevents premature degradation, thus resolving the contradiction between efficacy and stability.

Inventive Principle:
Principle #40Composite materials

Solution Approach 2:

The patent utilizes plant proteins as sacrificial carriers that are metabolically degraded after delivering borneol to the target site. These short-lived carrier molecules provide temporary stability during circulation and delivery, then are naturally broken down and eliminated, allowing the borneol to exert its full effect without long-term stability concerns.

Inventive Principle:
Principle #27Cheap short-living objects (Disposable)

3Productivity

If high concentration of borneol is used to maximize BBB-opening effect, then permeability increases, but side effects and toxicity increase

Engineering Contradiction:
ImproveBBB permeability enhancementVSAvoidtoxicity and side effects
Core Design Contradiction:
ProductivityVSObject-generated harmful factors

Solution Approach 1:

The patent achieves localized high concentration of borneol specifically at the blood-brain barrier interface through targeted delivery mechanisms, while maintaining low overall systemic concentration. This local quality approach allows maximum permeability enhancement at the target site without exposing the rest of the body to high concentrations that would cause toxicity, thus resolving the contradiction between efficacy and safety.

Inventive Principle:
Principle #3Local quality

Solution Approach 2:

The patent uses plant proteins as intermediary carriers that control the release and distribution of borneol. These intermediaries ensure borneol reaches the BBB at effective concentrations while being gradually released to avoid sudden high systemic exposure that would cause toxicity, thus balancing permeability enhancement with safety.

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 borneol-plant protein mixture, PB-154, effectively increases the bioavailability and brain targeting of drugs, potentially treating CNS disorders by facilitating the passage of bioactive compounds across the BBB, while being economically viable and environmentally friendly.

Implementation Method 1

borneol assisted the permeation of drugs across BBB and enhanced their distribution in the brain tissue

Methodology Applied
Scientific EffectPermeation enhancement: Permeation

Implementation Method 2

borneol can accelerate the absorption of gastrodin in the gastrointestinal tract and promote its distribution to the brain

Methodology Applied
Scientific EffectAbsorption enhancement: Absorption (physical)

Data Source

PatentEP3125915B1Process for preparing a powdered mixture of borneol and plant proteins to be used as dietary or food supplement, and related dietary or food supplement
Publication Date: 2020.11.25 BIOSFERED

AI summary

The present invention provides a process for preparing a powdered mixture of borneol and plant proteins. The process comprises the steps of providing a borneol solution in either acetone or ethyl alcohol, mixing the borneol solution with either cereal or non-cereal plant proteins at room temperature (20-24 °C), drying the mixture at room temperature (20-24 °C) and milling of the mixture in order to obtain a powder. Said powder comprising borneol and a plant protein is named PB-154. The method allows a tight binding of borneol with plant proteins. Also encompassed by the scope of the present invention is a dietary or food supplement (PB-154) to be used for the potential facilitation of the opening of the blood-brain barrier. Said property provides potentially improved healing effects of several natural and synthetic molecules.