Transnasal Blood-Brain Barrier Permeation Delivery

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Solution Overview

Problem

Current treatments for brain-related disorders, such as Alzheimer's and Parkinson's diseases, face challenges due to side effects from oral ingestion and the need for targeted delivery across the blood-brain barrier, with existing delivery methods not fully realizing their therapeutic potential.

Innovation Solution

A method involving transnasal administration of a first pharmaceutical agent to increase blood-brain barrier permeability, followed by targeted delivery of a second agent to specific brain regions, such as the sphenopalatine ganglion, using a device that sprays the agent laterally and superiorly to enhance the efficacy of CNS-acting pharmaceuticals.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If oral medicaments including cholinesterase-inhibiting pharmaceutical agents are used, then therapeutic response is achieved, but gastrointestinal side effects occur

Engineering Contradiction:
Improvetherapeutic responseVSAvoidgastrointestinal side effects
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent uses the nasal mucosa and olfactory nerve pathway as an intermediary route to deliver cholinesterase-inhibiting pharmaceutical agents directly to the brain, bypassing the gastrointestinal tract and avoiding associated side effects while maintaining therapeutic efficacy

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent replaces the oral ingestion route with transnasal delivery, substituting the gastrointestinal absorption mechanism with nasal mucosal absorption and olfactory nerve transport to achieve brain delivery without GI side effects

Inventive Principle:
Principle #28Mechanics substitution (Replace mechanical system)

2Object-affected harmful factors

If transnasal administration is used to avoid gastrointestinal side effects, then side effects are reduced, but targeted delivery to specific brain regions is not achieved

Engineering Contradiction:
Improvegastrointestinal side effectsVSAvoidtargeted delivery precision
Core Design Contradiction:
Object-affected harmful factorsVSManufacturing precision

Solution Approach 1:

The patent employs the olfactory nerve as a biological intermediary that naturally transports substances from the nasal cavity to specific brain regions, enabling targeted delivery without requiring complex mechanical targeting systems

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent changes the delivery route parameter from oral to transnasal, and further optimizes by targeting specific nasal regions (inferior turbinate, sphenopalatine ganglion area) to control the distribution pattern and achieve regional brain targeting

Inventive Principle:
Principle #35Parameter changes

3Ease of operation

If conventional transnasal delivery is used, then general mucosal absorption occurs, but specific region targeting (e.g., pterygopalatine ganglion) is not achieved

Engineering Contradiction:
Improvemucosal absorptionVSAvoidspecific region targeting
Core Design Contradiction:
Ease of operationVSManufacturing precision

Solution Approach 1:

The patent applies different delivery strategies to different nasal regions, specifically targeting the inferior turbinate and sphenopalatine ganglion area with precise spray positioning to achieve localized drug delivery to specific brain regions

Inventive Principle:
Principle #3Local quality

Solution Approach 2:

The patent adds spatial precision to transnasal delivery by positioning the spray device to target specific anatomical landmarks (inferior turbinate, sphenopalatine foramen area) and using angular positioning to direct medication to the pterygopalatine ganglion region

Inventive Principle:
Principle #17Another dimension (Dimensionality change)

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

This approach allows for effective reduction of symptoms in brain disorders at lower dosages, reducing side effects and improving treatment outcomes by temporarily increasing blood-brain barrier permeability, enabling targeted delivery of therapeutic agents across the barrier.

Implementation Method 1

transnasally administering to the subject a first pharmaceutical agent in an amount effective to increase blood-brain barrier permeability above an initial default permeability state to a second, more-permeable state

Methodology Applied
Scientific EffectPermeation: Permeation

Data Source

PatentUS10350189B2Method for transnasal delivery of blood-brain barrier permeation agent and therapeutic agent
Publication Date: 2019.07.16 XIA TIAN
  • US10350189B2 patent drawing
  • US10350189B2 patent drawing
  • US10350189B2 patent drawing

AI summary

Described herein is a method for treating a central nervous system disorder, said method comprising steps of first transnasally administering to or immediately adjacent the sphenopalatine ganglion a first pharmaceutical agent that effectively enhances permeability of the blood-brain barrier; and thereafter administering a second pharmaceutical agent with known efficacious value for action upon central nervous system tissue. The central nervous system disorder may be related directly to the brain or to other central nervous system tissues and cells.