Corticosteroid-Loaded Liposomes for Topical Injection

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Solution Overview

Problem

Current treatments for noninfectious anterior uveitis, such as steroid eye drops, suffer from poor ocular penetration, frequent administration requirements, and untargeted delivery, leading to inadequate inflammation control and steroid-related side effects like cataract and glaucoma.

Innovation Solution

Development of corticosteroid-loaded liposomes composed of non-charged vesicle-forming phospholipids with long-chain saturated fatty acids, administered subconjunctivally to directly target inflammatory cells, providing sustained intracellular release of corticosteroids.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If steroid eye drops are administered frequently to achieve desired anti-inflammatory effect, then inflammation control is improved, but patient compliance deteriorates and treatment burden increases

Engineering Contradiction:
Improveinflammation controlVSAvoidpatient compliance
Core Design Contradiction:
ReliabilityVSEase of operation

Solution Approach 1:

The liposomal formulation transforms the static, rapid-release characteristics of conventional steroid eye drops into a dynamic, sustained-release system. The liposomes gradually release corticosteroids over time, maintaining therapeutic levels without requiring frequent administration, thus improving patient compliance while maintaining inflammation control

Inventive Principle:
Principle #15Dynamics

Solution Approach 2:

The invention changes the release rate parameter of the corticosteroid by encapsulating it in liposomes. This transforms the rapid washout characteristic of free steroid eye drops into a slow, controlled release profile, extending the duration of action and reducing administration frequency from hourly to less frequent intervals

Inventive Principle:
Principle #35Parameter changes

2Reliability

If intensive steroid eye drop instillation is used to overcome poor ocular penetration, then therapeutic effect is improved, but drug loss to tear drainage increases

Engineering Contradiction:
Improvetherapeutic effectVSAvoiddrug loss
Core Design Contradiction:
ReliabilityVSLoss of substance

Solution Approach 1:

The liposomal formulation provides continuous drug delivery to the ocular surface and inflammatory cells. Instead of repeated bolus doses that are rapidly washed away, the liposomes continuously release corticosteroids at the target site, maintaining therapeutic action without requiring intensive instillation and minimizing drug loss to tear drainage

Inventive Principle:
Principle #20Continuity of useful action

Solution Approach 2:

The liposomes act as an intermediary carrier that protects the corticosteroid from rapid washout by tear drainage. The liposomal encapsulation allows the drug to bypass the limitation of tear flow, delivering the active ingredient directly to inflammatory cells while minimizing loss to drainage

Inventive Principle:
Principle #24Intermediary (Mediator)

3Area of stationary object

If untargeted steroid delivery is used to treat inflamed areas, then broad coverage is achieved, but steroid-related side effects increase

Engineering Contradiction:
Improvecoverage areaVSAvoidsteroid-related side effects
Core Design Contradiction:
Area of stationary objectVSObject-generated harmful factors

Solution Approach 1:

The liposomal formulation enables localized drug delivery specifically to inflammatory cells and affected tissues. The liposomes target and adhere to inflamed areas, releasing corticosteroids locally at the site of inflammation while minimizing exposure of healthy ocular tissues to the drug, thus reducing the risk of steroid-related side effects like cataract and glaucoma

Inventive Principle:
Principle #3Local quality

Solution Approach 2:

The liposomes serve as a targeted delivery vehicle that mediates between the corticosteroid and the inflammatory cells. This intermediary approach ensures the drug reaches the intended target (inflammatory cells) with high specificity, avoiding untargeted exposure of healthy tissues and thereby reducing harmful side effects

Inventive Principle:
Principle #24Intermediary (Mediator)

4Reliability

If conventional steroid eye drops are administered hourly to achieve adequate drug levels, then anti-inflammatory efficacy is improved, but treatment duration and time commitment increase

Engineering Contradiction:
Improveanti-inflammatory efficacyVSAvoidtreatment time
Core Design Contradiction:
ReliabilityVSLoss of time

Solution Approach 1:

The liposomal formulation introduces a dynamic, time-extending mechanism to drug delivery. The sustained-release特性 of liposomes extends the duration of therapeutic action from hours to days or weeks, transforming the treatment regimen from intensive hourly administration to much less frequent dosing while maintaining adequate drug levels and anti-inflammatory efficacy

Inventive Principle:
Principle #15Dynamics

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 achieves effective suppression of inflammation with reduced treatment frequency and lower side effects, as demonstrated by improved therapeutic outcomes and reduced incidence of steroid-related complications like cataract and glaucoma.

Implementation Method 1

Liposomes composed of non-charged vesicle-forming phospholipids, wherein said phospholipids comprise long-chain saturated fatty acids... comprising a corticosteroid in water-soluble form... providing sustained intracellular release of corticosteroids

Methodology Applied
Scientific EffectLiposomal encapsulation and cellular uptake:

Data Source

PatentEP3448359B1Liposomal corticosteroids for topical injection in inflamed lesions or areas
Publication Date: 2023.06.07 LAURENTIA HLDG BV
  • EP3448359B1 patent drawingFigure 1
  • EP3448359B1 patent drawingFigure 2~3
  • EP3448359B1 patent drawingFigure 4

AI summary

The invention relates to topical injection in inflamed lesions or areas with liposomal corticosteroids.