Journal
PHARMACEUTICS
Volume 13, Issue 10, Pages -Publisher
MDPI
DOI: 10.3390/pharmaceutics13101648
Keywords
photothermal therapy; near-infrared fluorescence imaging; tumor targeting; zwitterionic fluorophores; ZW800-1
Categories
Funding
- National Research Foundation of Korea (NRF) - Korea government (MSIT) [NRF-2021R1A2C1013465]
- Chonnam National University Hwasun Hospital - Research Institute of Clinical Medicine [HCRI20016, HCRI20017]
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ZW800-1 is a zwitterionic NIR fluorophore widely used in improved fluorescence imaging due to its balanced surface charges, but lacks tumor targetability, necessitating structural modifications. ZW800-AM, a tumor-targetable and renal-clearable analog developed based on structural modification, not only shows improved tumor targeting ability and a photothermal effect for killing tumor cells under 808 nm NIR laser irradiation, but also exhibits rapid renal elimination from the body within 4 hours of injection, similar to ZW800-1, making it a promising bifunctional phototherapeutic agent for tumor-targeted imaging and phototherapy.
ZW800-1, a representative zwitterionic near-infrared (NIR) fluorophore, can minimize background tissue uptake owing to its balanced surface charges, and therefore, is widely used for improved NIR fluorescence imaging. As ZW800-1 has no tumor targetability, tumor imaging is highly dependent on the ability of the molecules conjugated to the ZW800-1. To enable tumor targeting using ZW800-1 without additional conjugation, we developed a tumor-targetable and renal-clearable ZW800-1 analog (ZW800-AM) based on the structural modification of ZW800-1. Specifically, an amine group on the center linker of the ZW800-1 indocyanine backbone was modified by replacing phenoxypropionic acid with tyramine linkage on the meso-chlorine atom. This modification improved the tumor targeting ability, which is known as the structure-inherent targeting strategy. More importantly, ZW800-AM not only showed sufficient tumor accumulation without nonspecific uptake but also produced a photothermal effect, killing tumor cells under 808 nm NIR laser irradiation. In addition, ZW800-AM exhibited rapid renal elimination from the body within 4 h of injection, similar to ZW800-1. Overall, the discovery of ZW800-AM as a bifunctional phototherapeutic agent may provide an ideal alternative for tumor-targeted imaging and phototherapy.
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