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Abstract

Targeted delivery of therapeutic agents is of particular interest in the field of cancer treatment. However, there is an urgent need for developing clinically promising targeting approaches that can be readily administered in a green manner.

Methods: Five phthalocyanine derivatives bearing different anionic and cationic groups were designed and synthesized. Then, their binding affinity with albumin were studied using gel assays, optical spectra and computational simulation. Finally, in vitro and in vivo fluorescence imaging and photodynamic therapy (PDT) evaluations were carried out.

Results: The two positively charged compounds could selectively bind to albumin dimer over albumin monomer, while the three negatively charged phthalocyanines could bind to both albumin monomer and dimer. Following systemic administration, the phthalocyanines show improved tumor accumulation via transport by natural albumin. PDT evaluations indicate that one of the positively charged compounds, ZnPcN4, shows outstanding phototherapeutic efficacy against tumors in preclinical models.

Conclusion: Our findings demonstrate that the use of water-soluble phthalocyanines as photosensitizers and in vivo albumin as a natural carrier may provide a green and efficient approach for tumor-targeted imaging and therapy.

Author information

Xingshu Li1,2#, Keunsoo Jeong3#, Yoonji Lee4#, Tian Guo2, Dayoung Lee2, Jeongmin Park3, Nahyun Kwon2, Jung-Hyun Na2, Seung Kon Hong2, Sun-Shin Cha2, Jian-Dong Huang1✉, Sun Choi4✉, Sehoon Kim3,5, Juyoung Yoon2

1. College of Chemistry, State Key Laboratory of Photocatalysis on Energy and Environment, Fujian Provincial Key Laboratory of Cancer Metastasis Chemoprevention and Chemotherapy, Fuzhou University, Fuzhou 350108, China.
2. Department of Chemistry and Nano Science, Ewha Womans University, Seoul 03760, Republic of Korea.
3. Center for Theragnosis, Korea Institute of Science and Technology (KIST), Seoul 02792, Republic of Korea.
4. College of Pharmacy and Graduate School of Pharmaceutical Sciences, Ewha Womans University, Seoul 03760, Republic of Korea.
5. KU-KIST Graduate School of Converging Science and Technology, Korea University, Seoul 02841, Republic of Korea.
#These authors contributed equally to this work.