Optimization of the composition and production technology of cifelin stealth liposomes

摘要

Cifelin is a hydrophobic anticancer drug. It is recommended to use this drug in high doses in order to achieve a therapeutic effect. Unfortunately, this treatment leads to a number of side effects. Inclusion of the drug in stealth liposomes reduces the toxicity and ensures a long circulation of cifelin in the bloodstream. In this study, the optimum molar ratio of components (165:8:1) was found for liposomal membranes composed of phosphatidylcholine, cholesterol, and PEG-2000-DSPE, respectively. The possibilities of using liposome technology based on extrusion and sonication were compared. For cifelin liposomes with vesicle size about 150 +/- 10 nm, an entrapment efficiency of 98.3 % was estimated after sterilizing filtration of the dispersion. The liposome composition was confirmed by thin-layer chromatography with a mobile phase consisting of butanol:glacial acetic acid:water (12:3:5).