Abstract
The aim of our study was to discover an alternative active substance to tyrosine kinase inhibitors such as erlotinib (Erlo) used in lung cancer treatment and to develop an appropriate and efficient formulation for oral administration of the substance. Newly synthesized zinc (II) phthalocyanine bearing ferrocene groups (Pc-Zn) was chosen as a model drug due to its use in photodynamic therapy. Pc-Zn increased the amount of nicked form (Form II) by 22.90% and decreased the amount of supercoiled form (Form I) by 77.10% in DNA cleavage studies using plasmid pBR322 DNA in the presence of light and oxygen. Liposome formulations containing Pc-Zn (Pc-Zn Lip) or Erlo (Erlo Lip) had small particle size as 450.5±32.4 nm and 187.2±1.6 nm, respectively and coating with bovine serum albumin (BSA) had not significantly changed particle sizes. Pc-Zn loaded liposomes had significantly (p <0.001) cytotoxic effect under light irradiation than Erlo loaded liposomes. Coating with BSA had no significant effect on the cytotoxicity of the formulations. As a result, it was observed that Pc-Zn was more cytotoxic in the presence of light irradiation than Erlo. However, there was no significant difference in cytotoxic effects between the BSA-coated and non-coated Pc-Zn/Erlo formulations.
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