A phthalocyanine-based self-assembled nanophotosensitizer for efficient in vivo photodynamic anticancer therapy

• Published in: Journal of inorganic biochemistry 2021-04, Vol.217, p.111371-111371, Article 111371
• Main Authors: Lin, Ai-Lan, Chen, Jia-Hui, Hong, Jie-Wei, Zhao, Yuan-Yuan, Zheng, Bi-Yuan, Ke, Mei-Rong, Huang, Jian-Dong
• Format: Article
• Language: English
• Subjects: Animals; Antineoplastic Agents - chemical synthesis; Antineoplastic Agents - radiation effects; Antineoplastic Agents - therapeutic use; Cell Line, Tumor; Folic acid; Humans; Indoles - chemical synthesis; Indoles - radiation effects; Indoles - therapeutic use; Light; Mice; Nanophotosensitizer; Neoplasms - drug therapy; Photochemotherapy; Photodynamic therapy; Photosensitizing Agents - chemical synthesis; Photosensitizing Agents - radiation effects; Photosensitizing Agents - therapeutic use; Phthalocyanine; Rats; Self-assembly; Tumor-targeting
• ISSN: 0162-0134; 1873-3344
• DOI: 10.1016/j.jinorgbio.2021.111371

To develop highly efficient photosensitizers for photodynamic therapy, herein a zinc(II) phthalocyanine-folate conjugate (PcN-FA) used to construct an activatable nanophotosensitizer (NanoPcN-FA) through a facile self-assembly. The self-assembled nanophotosensitizer (NanoPcN) without folate-modification was used as a negative control. After self-assembly, the photoactivities of NanoPcN-FA was quenched. The in vitro studies showed that NanoPcN-FA could be taken in by folate-receptor (FR)-positive SKOV3 cells and activated in the cells. It also exhibited slightly higher photocytotoxicity against SKOV3 cells than NanoPcN. Moreover, the competitive assay confirmed that the cellular uptake of NanoPcN-FA was through a FR-mediated process. Finally, the in vivo results indicated that NanoPcN-FA could target tumor tissue of S180 rat ascitic tumor-bearing mice due to the folic acid (FA) ligand, leading to a highly efficient antitumor photodynamic efficacy with the tumor inhibition rate of 95%. [Display omitted] •A phthalocyanine-folate conjugate self-assembled into activatable nanophotosensitizer.•The photoactivities of the phthalocyanine were quenched in the nanophotosensitizer.•It was taken in by folate receptor (FR)-positive cells through a FR-mediated pathway.•The quenched photoactivities could be activated in FR-positive cells and tumor tissues.•It had efficient tumor targeting and in vivo photodynamic anticancer efficacy.