Cyanine Dimers for Stable Photothermal Therapy and Tumor Imaging

Resolve Bottlenecks,
Find Innovative SolutionsGenerate Solutions

Solution Overview

Problem

Cyanine derivatives used in photothermal therapy have limited photothermal activity, poor stability in aqueous solutions, and lack specific tumor targeting, failing to meet the requirements of both photoacoustic imaging and fluorescence imaging effectively.

Innovation Solution

Development of cyanine dimers with specific structural modifications, including phenyl or naphthyl groups, anions, and solubilizing or bioactive groups, to enhance stability, solubility, and targeting capabilities, allowing for effective photothermal therapy guided by fluorescence and photoacoustic imaging.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Power

If cyanine derivatives are used for photothermal therapy, then photothermal activity is achieved, but photothermal activity is limited and stability in aqueous solution is poor

Engineering Contradiction:

Improvephotothermal activityVSAvoidstability in aqueous solution

Core Design Contradiction:

PowerVSReliability

Solution Approach 1:

The patent creates cyanine dimers by coupling two cyanine molecules through a linker, forming a composite structure that combines the photothermal properties of cyanine with enhanced stability from the dimeric architecture and solubilizing groups

Inventive Principle:

Principle #40Composite materials

Solution Approach 2:

The patent modifies the molecular parameters of cyanine derivatives by introducing solubilizing groups (such as PEG chains, carbohydrate moieties, or charged groups) and forming dimers, which changes the physical and chemical parameters to improve aqueous stability while maintaining photothermal activity

Inventive Principle:

Principle #35Parameter changes

2Power

If cyanine derivatives are used for photothermal therapy, then treatment capability is achieved, but specific targeting of tumors is not enabled

Engineering Contradiction:

Improvephotothermal treatment capabilityVSAvoidtumor targeting capability

Core Design Contradiction:

PowerVSAdaptability or versatility

Solution Approach 1:

The cyanine dimer platform is designed as a multi-functional molecule that can simultaneously provide photothermal therapy, fluorescence imaging, and photoacoustic imaging, with the additional capability to attach various targeting moieties for different tumor types

Inventive Principle:

Principle #6Universality (Multi-functionality)

Solution Approach 2:

The patent uses linkers as intermediary structures that connect the cyanine chromophore to various bioactive moieties or targeting groups, enabling the same core structure to target different tumors through interchangeable targeting components

Inventive Principle:

Principle #24Intermediary (Mediator)

3Length of stationary object

If photoacoustic imaging and photothermal treatment are performed, then deep penetrability is achieved, but high fluorescence quantum yield is not required whereas fluorescence imaging requires it

Engineering Contradiction:

Improvepenetration depthVSAvoidfluorescence quantum yield requirement

Core Design Contradiction:

Length of stationary objectVSMeasurement precision

Solution Approach 1:

The patent designs cyanine dimers with dynamic fluorescence properties where the quantum yield can be modulated or optimized depending on the specific application, allowing the same compound to serve both photoacoustic imaging (where low quantum yield is acceptable) and fluorescence imaging (where high quantum yield is needed)

Inventive Principle:

Principle #15Dynamics

4Power

If cyanine derivatives are used, then photothermal activity is achieved, but stability under irradiation is poor

Engineering Contradiction:

Improvephotothermal activityVSAvoidstability under irradiation

Core Design Contradiction:

PowerVSDuration of action of stationary object

Solution Approach 1:

The dimeric structure and solubilizing groups act as protective elements that stabilize the cyanine chromophore against photodegradation before irradiation occurs, cushioning the molecule against harmful effects during prolonged exposure

Inventive Principle:

Principle #11Beforehand cushioning (Prior cushioning)

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 cyanine dimers exhibit significant photothermal activity, high signal strength in photoacoustic imaging, and improved stability under irradiation, enabling effective photothermal treatment and imaging of cancerous tumors.

Implementation Method 1

Photothermal treatment is a therapeutical approach based on light for the treatment of various cancers. This approach is based on a local increase of the temperature by irradiation of a photothermal agent (PTA) at a specific wavelength.

Methodology Applied

Scientific EffectPhotothermal conversion: Absorption (EM radiation)

Implementation Method 2

The photoacoustic imaging is a non-invasive technique based on the detection of photo-induced ultrasound signals.

Methodology Applied

Scientific EffectPhotoacoustic effect: Photoacoustic Effect

Implementation Method 3

Fluorescence imaging uses fluorophore absorbing and emitting in near-infrared.

Methodology Applied

Scientific EffectFluorescence: Fluorescence

Data Source

PatentEP4628546A1Cyanine dimers for photothermal treatment of cancer guided by fluorescence/photoacoustic imaging

Publication Date: 2025.10.08 CENT NAT DE LA RECH SCI (C N R S)

AI summary

The present invention relates to compounds of formula (I) and its use for photothermal therapy preferably for the treatment of cancer, for examples for the treatment of glioblastoma, prostate cancer, breast cancer and melanoma