Water-soluble phthalocyanines selectively bind to albumin dimers: A green approach toward enhancing tumor-targeted photodynamic therapy

Xingshu Li, Keunsoo Jeong, Yoonji Lee, Tian Guo, Dayoung Lee, Jeongmin Park, Nahyun Kwon, Jung Hyun Na, Seung Kon Hong, Sun Shin Cha, Jian Dong Huang, Sun Choi, Sehoon Kim, Juyoung Yoon

Research output: Contribution to journalArticlepeer-review

31 Scopus citations

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.

Original languageEnglish
Pages (from-to)6412-6423
Number of pages12
JournalTheranostics
Volume9
Issue number22
DOIs
StatePublished - 2019

Bibliographical note

Funding Information:
S.S.C. thanks the project titled “Development of biomedical materials based on marine proteins“, which were funded by the Ministry of Oceans and Fisheries (MOF).

Funding Information:
J.Y. thanks the National Research Foundation of Korea (NRF), which was funded by the Korea government (MSIP) (No. 2012R1A3A2048814). J.D.H. thanks National Natural Science Foundation of China (Grant Nos. U1705282, 21473033). S.K. thanks Korea Research Institute of Standards and Science (KRISS-2018-GP2018-0018) for KIST intramural program and the National Research Foundation of Korea (2017M3A9D8029942). S.C. thanks the National Research Foundation of Korea (NRF) grants, which were funded by the Korea government (MSIT) (No. 2018R1A5A2025286 and NRF-2017R1A2B4010084).

Funding Information:
J.Y. thanks the National Research Foundation of Korea (NRF), which was funded by the Korea government (MSIP) (No. 2012R1A3A2048814). J.D.H. thanks National Natural Science Foundation of China (Grant Nos. U1705282, 21473033). S.K. thanks Korea Research Institute of Standards and Science (KRISS-2018-GP2018-0018) for KIST intramural program and the National Research Foundation of Korea (2017M3A9D8029942). S.C. thanks the National Research Foundation of Korea (NRF) grants, which were funded by the Korea government (MSIT) (No. 2018R1A5A2025286 and NRF-2017R1A2B4010084). S.S.C. thanks the project titled ?Development of biomedical materials based on marine proteins?, which were funded by the Ministry of Oceans and Fisheries (MOF).

Publisher Copyright:
© The author(s).

Keywords

  • Albumin dimer
  • Natural carrier
  • Photodynamic therapy
  • Phthalocyanine
  • Tumor targeting

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