Introduction. The development of targeted delivery systems (DSs), including DSs with controlled release, e.g., photoinduced release, is considered to be one of the most promising directions of antitumour therapy development. The increasing morbidity of patients with non-small cell lung cancer makes it urgent to improve the therapy of this disease. One of the effective drugs in the treatment of this disease is Gefitinib (Gef); however, Gef is used in the form of tablets, and its bioavailability is about 50%. In this regard, the development of DSs with photoinduced release for Gefitinib is very promising, and their use will improve the safety profile of the drug and reduce undesirable effects.
Methods. The combined DSs were prepared by the following methods: 1. liposomes were obtained by the lipid film; 2. micelles were emulsified by inert gas bubbling. The created model formulations were evaluated according to the particle size, ζ-potential, and content of active substances. The cytotoxic activity of the nanoconstructions was studied on the lung carcinoma cell line A549.
Results. In the process work, model formulations of DSs with different morphologies were created. From the proposed formulations, the most promising ones were selected according to the criteria of particle size (˂200 nm) and active substance inclusion (85-90%). The leader models were also tested for cytotoxic activity on A549 cells. It turned out that only in the micellar model did the toxicity index for irradiated and non-irradiated cells exceed 50%. This indicates the promising application of this model for further research.
Conclusions. In the course of this work, biopharmaceutical studies were carried out to substantiate the composition and technology of targeted DSs with photoinduced release of Gefitinib and to study the antitumour activity in vitro.
Funding. This study was supported by the Russian Science Foundation grant No. 23-75-01026 «Development of targeted combined structures based on phospholipid nanosystems for lung cancer therapy».
