PEG-Lipid Nanoparticles for Blood-Brain Barrier Drug Delivery

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Solution Overview

Problem

Current treatments for neurodegenerative diseases like ALS face challenges in delivering therapeutic agents across the blood-brain and blood-spinal cord barriers due to efflux carriers and poor solubility of hydrophobic drugs, leading to limited efficacy and invasive delivery methods.

Innovation Solution

Development of therapeutic nanoparticles composed of poly(lactic) acid-poly(ethylene glycol) (PLA-PEG) copolymers or amphiphilic lipids, encapsulating biologically active ingredients such as adapalene, which are designed for controlled release and improved site-specific delivery to the central nervous system.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If hydrophobic drugs are used to treat neurodegenerative diseases, then therapeutic efficacy is improved, but solubility and delivery efficiency deteriorate

Engineering Contradiction:

Improvetherapeutic efficacyVSAvoidsolubility

Core Design Contradiction:

ReliabilityVSQuantity of substance

Solution Approach 1:

The patent employs PEG-lipids as intermediary molecules that bridge the hydrophobic drug and the aqueous environment. The PEG chain provides hydrophilicity for water solubility while the lipid tail anchors the hydrophobic drug, enabling both solubility and therapeutic efficacy

Inventive Principle:

Principle #24Intermediary (Mediator)

Solution Approach 2:

The invention creates composite nanoparticle structures combining PEG-lipids with hydrophobic drugs. This composite approach allows the system to simultaneously exhibit properties of both hydrophilic (for solubility) and hydrophobic (for drug loading and efficacy) components

Inventive Principle:

Principle #40Composite materials

2Productivity

If lipophilic drugs are used to cross the blood-brain barrier, then delivery efficiency is improved, but solubility and tissue penetration deteriorate

Engineering Contradiction:

Improvedelivery efficiencyVSAvoidsolubility

Core Design Contradiction:

ProductivityVSQuantity of substance

Solution Approach 1:

PEG-lipids serve as mediators that enable lipophilic drugs to achieve both brain delivery and solubility. The amphiphilic structure of PEG-lipids creates a bridge between the lipophilic drug and the aqueous bloodstream, facilitating transport across the blood-brain barrier while maintaining solubility

Inventive Principle:

Principle #24Intermediary (Mediator)

3Productivity

If efflux carriers are present in the blood-brain barrier, then drug transport out of cells is improved, but therapeutic delivery into the brain deteriorates

Engineering Contradiction:

Improvedrug transport efficiencyVSAvoidtherapeutic delivery

Core Design Contradiction:

ProductivityVSReliability

Solution Approach 1:

The PEG-lipid nanoparticle acts as an intermediary delivery vehicle that bypasses the efflux carrier mechanism. By encapsulating the drug in a PEG-lipid complex, the system avoids recognition by P-glycoprotein efflux pumps, enabling successful brain delivery

Inventive Principle:

Principle #24Intermediary (Mediator)

Data Source

PatentUS11446267B2Nanoparticle compositions, methods of fabrication, and use for drug delivery

Publication Date: 2022.09.20 DIGNITY HEALTH

AI summary

The invention relates to a composition and use of the composition in the treatment of a disorder, for example, a neurological disease associated with retinoid signaling. The invention also includes the use of a retinoid encapsulated in nanoparticles. The retinoid encapsulated nanoparticles are adapted to increasing lifespan and conferring neuroprotective effects such as preserving motor units, reducing motor impairment, or reducing neuroinflammation in a subject.