Nanostructured Carrier Systems with Polymethine Dyes for Tissue Targeting

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Solution Overview

Problem

Current nanoparticle-based drug delivery systems for targeting specific tissues, such as the liver or kidney, suffer from non-selective and passive transport mechanisms, leading to unintended side effects and limited efficacy, as they do not enable active and selective accumulation of pharmaceutical active ingredients in target tissues.

Innovation Solution

A nanostructured carrier system comprising polymers and/or lipids conjugated with polymethine dyes, which act as targeting units to selectively transport pharmaceutical active ingredients into specific tissues by interacting with tissue-specific transporters, allowing for active and selective accumulation and release within the target tissue.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of manufacture

If passive transport mechanisms are used for nanoparticle delivery, then the system is simple and easy to manufacture, but the transport is non-selective leading to systemic side effects

Engineering Contradiction:
Improveease of manufactureVSAvoidsystemic side effects
Core Design Contradiction:
Ease of manufactureVSObject-affected harmful factors

Solution Approach 1:

The patent applies local quality by equipping nanoparticles with specific targeting ligands (antibodies, peptides, or small molecules) on their surface that recognize and bind to specific receptors or transporters only in the target tissue. This creates localized specificity without changing the overall nanoparticle structure or manufacturing process significantly, resolving the contradiction between ease of manufacture and reduction of systemic side effects.

Inventive Principle:
Principle #3Local quality

Solution Approach 2:

The patent uses targeting ligands as intermediaries between the nanoparticle and the target tissue. These ligands act as mediators that facilitate selective recognition and binding to tissue-specific receptors or transporters, enabling selective transport without requiring complex changes to the nanoparticle core or manufacturing process.

Inventive Principle:
Principle #24Intermediary (Mediator)

2Ease of manufacture

If passive EPR effect transport is used, then the nanoparticle can be manufactured simply, but the accumulation is limited to tumor tissue only

Engineering Contradiction:
Improveease of manufactureVSAvoidtissue targeting versatility
Core Design Contradiction:
Ease of manufactureVSAdaptability or versatility

Solution Approach 1:

The patent applies local quality by functionalizing the nanoparticle surface with interchangeable targeting ligands that can be selected to match different tissue-specific receptors or transporters. This allows the same nanoparticle platform to be adapted for different target tissues (liver, kidney, tumor, etc.) without changing the core manufacturing process, thus resolving the contradiction between ease of manufacture and tissue targeting versatility.

Inventive Principle:
Principle #3Local quality

Solution Approach 2:

The patent implements universality by creating a modular nanoparticle platform where the core structure and manufacturing process remain constant, but the surface targeting ligands can be exchanged to target different tissues. This multi-functional approach allows a single nanoparticle design to serve multiple tissue-specific delivery applications.

Inventive Principle:
Principle #6Universality (Multi-functionality)

3Reliability

If active targeting with antibodies is used, then selectivity is improved, but the device complexity and manufacturing difficulty increase

Engineering Contradiction:
ImproveselectivityVSAvoiddevice complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent applies parameter changes by using small molecule targeting ligands instead of large antibodies. These small molecules have different physical and chemical parameters (smaller size, higher stability, easier synthesis) that simplify the overall system while maintaining or improving selectivity through high-affinity binding to specific tissue receptors or transporters.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent uses small molecule targeting ligands that are chemically synthesizable and more stable than antibodies. These ligands can be produced more cheaply and with greater consistency, reducing device complexity and manufacturing difficulty while maintaining reliable tissue-specific targeting.

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

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 enables efficient, targeted delivery of pharmaceutical active ingredients to specific tissues, reducing systemic side effects and enhancing therapeutic efficacy while allowing for monitoring and tracking through fluorescence properties, thereby improving treatment outcomes for liver and kidney diseases.

Implementation Method 1

the coupled dyes, usually fluorescent dyes such as cyanines, are used as markers whose fluorescence and absorption properties are measured

Methodology Applied
Scientific EffectFluorescence: Fluorescence

Implementation Method 2

the dye is used as a marker in a tissue or a body fluid, such as blood or urine, and is excited radiatively. The fluorescence emission of the dye is then detected

Methodology Applied
Scientific EffectAbsorption (EM radiation): Absorption (EM radiation)

Data Source

PatentEP2848262B1Cell-specific targeting by nanostructured carrier systems
Publication Date: 2020.11.04 SMARTDYELIVERY
  • EP2848262B1 patent drawingFigure 1
  • EP2848262B1 patent drawingFigure 2A~2B
  • EP2848262B1 patent drawingFigure 3A~3C

AI summary

The invention relates to a nanostructured carrier system comprising at least one polymer and/or at least one lipid and at least one polymethine dye, wherein the at least one polymethine dye acts as a targeting unit to effect the targeted transport of the nanostructured carrier system into a target tissue. The invention further relates to pharmaceutical compositions and uses of the nanostructured carrier system for transporting the same and optionally a pharmaceutical active ingredient into a target tissue, as well as for treating diseases of the liver and/or kidney.