PEG-Conjugated Near-Infrared Dye for Tumor Accumulation
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Solution Overview
Problem
Existing near-infrared organic dyes, such as indocyanine green, have a low tumor accumulation rate, which limits their effectiveness as contrast agents for optical imaging, particularly in visualizing tumors.
Innovation Solution
A compound with at least one organic dye covalently bound to polyethylene glycol, represented by a specific formula, is developed to enhance tumor accumulation, incorporating a dispersion medium and potentially a capturing molecule for targeted imaging.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Quantity of substance
If conventional near-infrared organic dyes (e.g., indocyanine green) are used as contrast agents, then the imaging method can be implemented, but the tumor accumulation rate is low
Solution Approach 1:
The patent applies composite materials by combining near-infrared organic dyes with polyethylene glycol (PEG) chains to create a new contrast agent compound. This composite structure leverages the optical properties of the dye and the tumor-targeting capabilities of PEG, achieving both high tumor accumulation and effective imaging. The compound consists of a dye molecule covalently bonded to PEG chains, forming a hybrid material that solves the low accumulation problem of conventional dyes.
Solution Approach 2:
The patent employs parameter changes by modifying the molecular structure of the contrast agent through varying PEG chain lengths (n1 and n2 in the formula), dye molecule substitutions (R1-R14 groups), and conjugation methods. These parameter adjustments optimize the compound's hydrophilicity, molecular weight, and tumor penetration capabilities, thereby enhancing tumor accumulation rate while maintaining imaging performance.
2Quantity of substance
If functional groups are introduced to the methine chain portion of the near-infrared organic dye, then tumor accumulation rate may improve, but the dye's inherent optical properties may be compromised
Solution Approach 1:
The patent applies local quality by introducing functional groups and PEG chains at specific locations on the dye molecule (at the methine chain portions with R1-R14 substituents) rather than modifying the entire molecule uniformly. This localized modification allows the core chromophore structure to retain its optical properties while the peripheral functional groups provide tumor-targeting capabilities through the EPR effect.
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 compound achieves a higher tumor accumulation rate and retention, allowing for improved visualization of tumors and lymph nodes through enhanced permeability and retention effects, with a higher tumor-to-blood ratio, thereby facilitating more effective optical imaging.
Implementation Method 1
a signal, such as an acoustic wave and fluorescence, emitted from a substance (light absorber) that absorbs light in a specimen in irradiation of the specimen with light is measured for imaging
Implementation Method 2
A technique where a subject is irradiated with light and the acoustic wave is measured for imaging is referred to as photoacoustic imaging
Implementation Method 3
The compound achieves a higher tumor accumulation rate and retention, allowing for improved visualization of tumors and lymph nodes through enhanced permeability and retention effects
Data Source
AI summary
A compound having a high tumor accumulation rate, or a salt thereof, and a contrast agent for optical imaging are provided. A compound having at least one specific organic dye covalently bound to polyethylene glycol, or a salt thereof is provided.


