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.

我们研究的目的是发现可替代酪氨酸激酶抑制剂（如埃洛替尼（Erlo））用于肺癌治疗的活性物质，并开发出一种合适且有效的口服制剂。由于新合成的带有二茂铁基团的锌（II）酞菁锌（Pc-Zn）被选作模型药物，因为它在光动力疗法中得到了应用。在存在光和氧的情况下，使用质粒pBR322 DNA进行的DNA切割研究中，Pc-Zn使切刻形式（形式II）的量增加了22.90％，使超螺旋形式（形式I）的量减少了77.10％。含有Pc-Zn（Pc-Zn Lip）或Erlo（Erlo Lip）的脂质体制剂分别具有450.5±32.4 nm和187.2±1.6 nm的小粒径，并且涂有牛血清白蛋白（BSA）的粒径没有明显变化。p <0.001）在光照射下比Erlo脂质体具有细胞毒性作用。用BSA包衣对制剂的细胞毒性没有显着影响。结果，观察到在有光照射的情况下，Pc-Zn比Erlo更具细胞毒性。但是，在BSA涂层和未涂层​​的Pc-Zn / Erlo制剂之间，在细胞毒性作用方面没有显着差异。