Liposomal forms of new antitumor drugs based on europium chelates examined by P-terphenyl fluorescence quenching

Abstract

Europium chelates have been previously shown to possess pronounced cytotoxic activity. These compounds are of great interest for biomedical investigations and diagnostics, because their spectral characteristics are optimal for visualization of the occurred processes. Application of these pharmaceutical compounds in the free form is limited by their high toxicity and metabolic instability. In view of this, the development of the delivery systems for europium chelates becomes actual. Liposomes represent one of the most promising delivery systems, which allows to increase the efficiency of pharmacological agents. The use of liposomal formulations of antitumor drugs is currently in a focus of biomedical and biophysical research due to the following advantages: complete biocompatibility, ability to carry both lipophilic and hydrophilic compounds, protecting them from chemical degradation and transformation, decreased toxicity and increased therapeutic index of drug, etc. In the present work we explore the interaction between europium chelates (here referred to as V6 and V8) and model lipid membranes. Fluorescence intensity of membrane-incorporated probe p-terphenyl was found to decrease with enhancement of drugs concentration. The obtained results indicate that p-terphenyl fluorescence is quenched upon europium chelate incorporation into phosphatidylcholine liposomes. Quantitative characteristics of p-terphenyl fluorescence quenching by the drugs under consideration have been determined.