Investigation of In vitro PDT Activities and In vivo Biopotential of Zinc Phthalocyanines Using ¹³¹I Radioisotope

Abstract

Novel octylthio-containing asymmetrically substituted Zn(II) phthalocyanine (Zn(II)Pc1) and a symmetric derivative (Zn(II)Pc2) have been prepared to investigate the biological potential and ability to photosensitize singlet oxygen for photodynamic therapy applications. In this study, the singlet oxygen generation potential and in vitro photodynamic activities of these compounds have been tested. Both ZnPcs reveal to be very efficient singlet oxygen generators and promising PSs for PDT applications. In vitro PDT activities of the compounds were evaluated in EMT-6 murine mammary carcinoma and HeLa human cervix carcinoma cell lines. Moreover, Zn(II)Pc1 displayed the phototoxic effects in the mammary cancer cell line (6.25 μm concentration at 30 J/cm(2) light dose and 12.5 μm concentration at 20 J/cm(2) light dose), while Zn(II)Pc2 did not show any phototoxic effects both in two cell lines. Zn(II)Pcs were radiolabeled with (131) I in high yields. Biodistribution studies revealed that the radiolabeled Zn(II)Pc1 showed significant uptake in l. intestine, pancreas, brain, and ovary, while Zn(II)Pc2 has significant uptake in ovary and pancreas in normal rats. Hence, these Pcs derivatives could be promising candidate for tumor nuclear imaging.

Phototoxicity of Liposomal Zn- and Al-phthalocyanine Against Cervical and Oral Squamous Cell Carcinoma Cells In Vitro

“…The effect of non-liposomal AlPc and ZnPc was not reported in these studies. PDT efficacy of the symmetric derivative Zn(II)Pc 1 and asymmetrically substituted ZnPc(II) 2 have been investigated in mouse mammary carcinoma EMT6/P cells and HeLa cervical adenocarcinoma cells [ 49 , 50 ]. Zn(II)Pc 1 was photocytotoxic in EMT6/P cells (IC 50 ~3.14 μM) but not in HeLa cells, whereas Zn(II)Pc 2 was not phototoxic in EMT6/P cells but was photoactive in HeLa cells (IC 50 ~3.13 μM at 30 J/cm 2 ).…”

Photodynamic therapy and nuclear imaging activities of zinc phthalocyanine‐integrated TiO2 nanoparticles in breast and cervical tumors

“…The photodynamic therapy efficacies of ZnPc, ZnPc‐TiO 2 , and TiO 2 have been evaluated in control group that non‐cytotoxicity at concentrations of 1.57, 3.13, and 6.25 μ m without phototherapy (PT‐). The phototoxicities of ZnPc, ZnPc‐TiO 2 , and TiO 2 were determined according to the untreated control group in which the substance was not applied and the light was applied …”

Photosensitizers for Photodynamic Therapy of Brain Cancers—A Review

“…Biodistribution studies revealed that radiolabeled Zn(II)Pc1 showed significant uptake in the brain, intestine, pancreas and ovary. Hence, these Pcs derivatives could also be promising candidates for the nuclear imaging of tumors [ 109 ].…”