Microcapsule Hydrogel Sustained Release for Mental Illness

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Solution Overview

Problem

Current drug delivery systems for mental illnesses and central nervous system disorders face challenges in maintaining a consistent drug concentration over time, leading to excessive initial drug release and reduced efficacy due to rapid drug release rates, which complicates treatment and increases side effects.

Innovation Solution

A sustained-release drug delivery formulation using microcapsules containing biodegradable polymers and crosslinked hydrogels, specifically with methyltetrazine-PEG4-NHS ester and trans-cyclooctene-NHS ester or amine, to control the release of psychopharmaceutical agents like aripiprazole and donepezil, ensuring a constant drug level over a long period.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If a drug at a relatively high concentration is administered at one time, then the immediate therapeutic effect is improved, but a dose-dependent side effect frequently occurs

Engineering Contradiction:
Improvetherapeutic effectVSAvoidside effect
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent segments the total drug dose into multiple smaller releases over time using a sustained-release formulation. The drug is encapsulated in a matrix that gradually releases it, converting a single high-concentration administration into multiple low-concentration releases, thereby maintaining therapeutic effect while avoiding dose-dependent side effects

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The patent employs preliminary action by pre-encapsulating the drug in a sustained-release matrix before administration. This preliminary structuring ensures that the drug is automatically released at controlled rates over time, preventing the need for repeated high-dose administrations and their associated side effects

Inventive Principle:
Principle #10Preliminary action

2Object-affected harmful factors

If the concentration of a drug is reduced to a predetermined level or less between administrations of the drug, then side effects are reduced, but the administration efficacy deteriorates and the period during which a patient adapts to the drug may be prolonged

Engineering Contradiction:
Improveside effectVSAvoidadministration efficacy
Core Design Contradiction:
Object-affected harmful factorsVSReliability

Solution Approach 1:

The patent ensures continuity of useful action by designing a sustained-release system that maintains drug concentration within the therapeutic window continuously over time. The controlled release mechanism prevents concentration from dropping below effective levels between administrations, thereby maintaining administration efficacy while keeping side effects minimal

Inventive Principle:
Principle #20Continuity of useful action

3Productivity

If a sustained release formulation is developed, then the administration frequency is reduced and therapeutic blood or tissue level of the drug may be maintained for an extended period of time, but the formulation complexity increases

Engineering Contradiction:
Improveadministration frequencyVSAvoidformulation complexity
Core Design Contradiction:
ProductivityVSDevice complexity

Solution Approach 1:

The patent applies parameter changes by modifying the physical and chemical properties of the drug delivery system. By changing the matrix composition, porosity, and degradation rate parameters, the formulation achieves sustained release functionality without requiring complex mechanical structures or multiple components, thereby reducing formulation complexity while maintaining extended therapeutic levels

Inventive Principle:
Principle #35Parameter changes

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 formulation achieves a controlled, sustained release of drugs, reducing initial burst release and maintaining therapeutic blood levels, thereby enhancing treatment efficacy and reducing the need for frequent administrations, while simplifying the preparation process and lowering costs.

Implementation Method 1

a microcapsule in which a psychopharmaceutical agent or an antidepressant is contained in a biodegradable polymer

Methodology Applied
Scientific EffectHydrolysis: Hydrolysis

Implementation Method 2

a hydrogel in which a material including a first chemical functional group and a material including a second chemical functional group are crosslinked to each other

Methodology Applied
Scientific EffectAbsorption: Absorption (physical)

Data Source

PatentEP3581175B1Drug drug delivery formulation for treating mental illness or central nervous system disorder
Publication Date: 2023.12.13 AJOU UNIV IND ACADEMIC COOP FOUND
  • EP3581175B1 patent drawingFigure 1
  • EP3581175B1 patent drawingFigure 2
  • EP3581175B1 patent drawingFigure 3

AI summary

The present invention relates to a drug delivery formulation for treating a mental illness or a central nervous system disorder and, more particularly, to a drug delivery formulation for treating a mental illness or a central nervous system disorder, comprising a microcapsule containing a biodegradable polymer and a drug and a crosslinked hydrogel and a method for preparing the same. A drug delivery formulation for treating a mental illness or a central nervous system disorder according to the present invention can slowly release a drug at a constant rate without a burst of drug release in the early stage of drug administration to maintain a constant blood drug level over a long period of time and thus enjoys the advantage of preventing excessive initial release of drug, which is a problem with the administration of conventional psychopharmaceutical agents or antidepressants, and easily obtaining a desirable sustained release behavior by single administration without necessity for multiple administrations divided at regular time intervals. In addition, a method for preparing a drug delivery formulation according to the present invention is a process simpler than conventional methods and has the advantage of reducing time and cost in preparing a sustained-release drug delivery formulation.