Intracellular uptake and fluorescence imaging potential in tumor cell of zinc phthalocyanine

Int J Pharm. 2016 May 30;505(1-2):369-75. doi: 10.1016/j.ijpharm.2016.04.023. Epub 2016 Apr 13.

Abstract

A near IR absorbing phthalocyanine bearing four binaphtyl group has been synthesized in order to investigate its cytotoxicity and intracellular uptake of sensitizer on MCF-7 (human breast cancer), MDAH (ovarian cancer), HeLa (human epitheloid cervix carcinoma), EMT-6 (mouse breast cancer) and WI-38 (human fibroblast lung) cell lines. ZnPc showed four time higher intracellular uptake in carcinoma cells (MCF-7) than normal (WI-38) cell lines. With the aim of studying in detail the biodistribution feature and tumor nuclear imaging capacity, ZnPc was also labeled with I-131. The efficiency of radiolabeled compound was 95±4.6%. In addition, ZnPc reveals to be very efficient singlet oxygen generators (ΦΔ=0.612 in DMSO) and promising PS for PDT application. In vitro fluorescence imaging study with MCF-7 cells showed that ZnPc localized in cytoplasm of the cells. This results showed that synthesized ZnPc is promising candidate for dual fluorescence/nuclear imaging breast cancer and shows potential PS for PDT application.

Keywords: (131)I; Breast cancer; Dual imaging; Nuclear imaging; Phthalocyanine; Radiolabeling.

MeSH terms

  • Animals
  • Breast Neoplasms / metabolism
  • Cell Line, Tumor
  • Cytoplasm / metabolism
  • Female
  • Humans
  • Indoles / administration & dosage*
  • Indoles / chemical synthesis
  • Indoles / pharmacokinetics
  • Iodine Radioisotopes
  • Isoindoles
  • MCF-7 Cells
  • Mice
  • Optical Imaging / methods
  • Organometallic Compounds / administration & dosage*
  • Organometallic Compounds / chemical synthesis
  • Organometallic Compounds / pharmacokinetics
  • Photochemotherapy / methods*
  • Photosensitizing Agents / administration & dosage*
  • Photosensitizing Agents / chemical synthesis
  • Photosensitizing Agents / pharmacokinetics
  • Singlet Oxygen / metabolism
  • Tissue Distribution
  • Zinc Compounds

Substances

  • Indoles
  • Iodine Radioisotopes
  • Isoindoles
  • Organometallic Compounds
  • Photosensitizing Agents
  • Zinc Compounds
  • Zn(II)-phthalocyanine
  • Singlet Oxygen