ZW800‐PEG: A Renal Clearable Zwitterionic Near‐Infrared Fluorophore for Potential Clinical Translation. Issue 25 (17th May 2021)

• Record Type: Journal Article
• Authors: Yang, Chengeng; Wang, Haoran; Yokomizo, Shinya; Hickey, Morgan; Chang, Hyejin; Kang, Homan; Fukuda, Takeshi; Song, Mi Young; Lee, Sang Yeul; Park, Jin Woo; Bao, Kai; Choi, Hak Soo
• Is Part Of: Angewandte Chemie international edition. Volume 60:Issue 25(2021)
• Page Start: 13847
• Page End: 13852
• Publication Date: 2021-05-17
• Subjects: minimal toxicity -- photothermal therapy -- renal clearance -- serum stability -- zwitterionic fluorophores; Chemistry -- Periodicals; 540
• DOI: 10.1002/anie.202102640
• Languages: English
• ISSNs: 1433-7851

Abstract

Abstract: Near‐infrared (NIR) fluorescence imaging has advanced medical imaging and image‐guided interventions during the past three decades. Despite tremendous advances in imaging devices, surprisingly only a few dyes are currently available in the clinic. Previous fluorophores, ZW800‐1A and ZW800‐1C, significantly improved the poor performance of the FDA‐approved indocyanine green. However, ZW800‐1A is not stable in serum and ZW800‐1C induces severe stacking in aqueous media. To solve such dilemmas, ZW800‐PEG was designed by introducing a flexible yet stable thiol PEG linker. ZW800‐PEG shows high solubility in both aqueous and organic solvents, thus improving renal clearance with minimal binding to serum proteins during systemic circulation. The sulfide group on the meso position of the heptamethine core improves serum stability and physicochemical properties including the maximum emission wavelength shift to 800 nm, enabling the use of ZW800‐PEG for image‐guided interventions and augmenting photothermal therapy. Abstract : ZW800‐PEG is a water‐soluble, non‐sticky, and renal clearable near‐infrared fluorophore owing to the balanced zwitterionic charges. By introducing a stable sulfide linker, it improves serum stability and also exhibits potential for augmenting photothermal therapy. It shows a maximum emission wavelength at 800 nm, enabling its use for image‐guided interventions in the OR using conventional near‐infrared imaging systems.