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ZW800-PEG: A Renal Clearable Zwitterionic Near-Infrared Fluorophore for Potential Clinical Translation
Chengeng Yang1, Haoran Wang1,2, Shinya Yokomizo1
1Gordon Center for Medical Imaging, Department of Radiology, Massachusetts General Hospital and Harvard Medical School, Boston, MA, 02129, USA.
Angewandte Chemie (International Ed. in English)
|April 15, 2021
Summary
A new near-infrared (NIR) dye, ZW800-PEG, offers improved serum stability and solubility for enhanced medical imaging. This novel fluorophore advances image-guided interventions and photothermal therapy applications.
Area of Science:
- Medical Imaging
- Biomedical Engineering
- Organic Chemistry
Background:
- Near-infrared (NIR) fluorescence imaging is crucial for medical diagnostics and image-guided interventions.
- Current clinical NIR dyes, like indocyanine green, have limitations in performance and stability.
- Previous ZW800 series dyes showed promise but suffered from serum instability (ZW800-1A) or aggregation (ZW800-1C).
Purpose of the Study:
- To develop a novel NIR fluorophore with enhanced stability and solubility for improved clinical applications.
- To address the limitations of existing NIR dyes, specifically serum instability and aggregation.
- To create a versatile dye suitable for both diagnostic imaging and therapeutic interventions.
Main Methods:
- Design and synthesis of ZW800-PEG by incorporating a thiol polyethylene glycol (PEG) linker.
- Evaluation of ZW800-PEG's solubility in aqueous and organic solvents.
- Assessment of serum stability and protein binding during systemic circulation.
- Characterization of physicochemical properties, including maximum emission wavelength.
Main Results:
- ZW800-PEG exhibits high solubility in both aqueous and organic media.
- The dye demonstrates improved serum stability due to a sulfide group on the heptamethine core.
- ZW800-PEG shows minimal binding to serum proteins, facilitating renal clearance.
- A maximum emission wavelength shift to 800 nm was observed, suitable for deep tissue imaging.
Conclusions:
- ZW800-PEG represents a significant advancement over previous NIR fluorophores, overcoming issues of instability and aggregation.
- Its enhanced physicochemical properties make it ideal for image-guided interventions.
- The dye holds potential for augmenting photothermal therapy, expanding its clinical utility.
