Journal
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
Volume 23, Issue 22, Pages -Publisher
MDPI
DOI: 10.3390/ijms232214093
Keywords
chlorambucil; zwitterionic fluorophores; near-infrared fluorescence imaging; photothermal therapy; tumor targeting
Funding
- National Research Foundation of Korea (NRF) - Korea government (MSIT) [NRF-2021R1A2C1013465]
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This study developed a feasible strategy for improving tumor targeting, in vivo biodistribution, and photothermal therapy (PTT) performance by conjugating a water-insoluble anticancer drug with a highly water-soluble zwitterionic near-infrared (NIR) fluorophore. The results demonstrated high tumor accumulation and rapid body clearance behavior, as well as effective photothermal therapy for cancer treatment.
Improving the tumor targeting of anticancer drugs to minimize systemic exposure remains challenging. The chemical conjugation of anticancer drugs with various near-infrared (NIR) fluorophores may provide an effective approach to improve NIR laser-induced cancer phototherapy. Towards this end, the selection of NIR fluorophores conjugated with hydrophobic anticancer drugs is an important consideration for targeted cancer photothermal therapy (PTT). In this study, a highly water-soluble zwitterionic NIR fluorophore (ZW800) was prepared to conjugate with a water-insoluble anticancer drug, chlorambucil (CLB), to improve tumor targeting, in vivo biodistribution, and PTT performance. The in vivo results using an HT-29 xenograft mouse model demonstrated that the CLB-ZW800 conjugate not only exhibited high tumor accumulation within 4 h after injection, but also showed rapid body clearance behavior for less systemic toxicity. Furthermore, the tumor tissue targeted by the CLB-ZW800 conjugate was exposed to 808 nm NIR laser irradiation to generate photothermal energy and promote apoptotic cell death for the effective PTT of cancer. Therefore, this study provides a feasible strategy for developing bifunctional PTT agents capable of tumor-targeted imaging and phototherapy by the conjugation of small molecule drugs with the versatile zwitterionic NIR fluorophore.
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