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
Engineering 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
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.
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.
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
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.
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.
3Reliability
If active targeting with antibodies is used, then selectivity is improved, but the device complexity and manufacturing difficulty increase
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.
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.
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
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
Data Source
Figure 1
Figure 2A~2B
Figure 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.