131I-Zn-Chlorophyll derivative photosensitizer for tumor imaging and photodynamic therapy

Int J Pharm. 2015 Sep 30;493(1-2):96-101. doi: 10.1016/j.ijpharm.2015.07.047. Epub 2015 Jul 28.

Abstract

In recent years, the photodynamic therapy studies have gained considerable attention as an alternative method to surgery, chemotherapy and radiotherapy which is commonly used to fight cancer. In this study, biological potentials of a benzyloxy bearing zinc(II) pheophorbide-a (Zn-PH-A) were investigated via in vivo and in vitro experiments. Zn-PH-A was labeled with (131)I with high efficiency (95.3 ± 2.7%) and its biodistribution studies were investigated on female Albino Wistar rats. The radiolabeled photosensitizer had been intravenously injected into the tail vein, and then the animals were sacrificed at 30, 60 and 120 min post injection. The percent of radioactivity per gram of organs (%ID/g) was determined. The radiolabeled Zn-PH-A showed high uptake in ovary. In addition, photodynamic therapy studies of the photosensitizer were conducted in EMT6, murine mammary carcinoma and HeLa, human cervix carcinoma cell lines. For the photodynamic therapy studies, the cells with Zn-PH-A were exposed to red light (650 nm) at the doses of 10-30 J/cm(2). The results showed that Zn-PH-A has stronger PDT effect in EMT6 than HeLa cell. Our present work demonstrates (131)I-labeled photosensitizer as a bifunctional agent (PDT and nuclear imaging) which could be improved in future by using EMT6 growing tumor in nude mice.

Keywords: (131)I; Biodistribution; Cancer; Chlorophyll; Photodynamic therapy; Radiolabeling.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Cell Line, Tumor
  • Chemistry, Pharmaceutical
  • Chlorophyll / analogs & derivatives*
  • Chlorophyll / chemistry
  • Chlorophyll / pharmacokinetics
  • Chlorophyll / pharmacology
  • Female
  • HeLa Cells
  • Humans
  • Hydrogen-Ion Concentration
  • Iodine Radioisotopes
  • Mice
  • Photochemotherapy / methods*
  • Photosensitizing Agents / pharmacokinetics
  • Photosensitizing Agents / pharmacology*
  • Rats
  • Rats, Wistar
  • Zinc / chemistry
  • Zinc / pharmacokinetics
  • Zinc / pharmacology*

Substances

  • Iodine Radioisotopes
  • Photosensitizing Agents
  • Chlorophyll
  • pheophorbide a
  • Zinc