Effect of long-term stabilization of cationic liposomes as defibrotide delivery system for antithrombotic activity

Abstract

The goal of the study was to produce cationic liposome formulations for the in vivo administration of the polydesoxyribonucleotide defibrotide and to investigate the in vivo ability of the liposomes to control hypertension. Liposomes were produced by the reverse phase evaporation method and extruded through policarbonate filters with pores of precalibrated diameter. Liposomes were then lyophilized by the presence of lyo- or cryo-protectants such as saccharides, dissolved in the dispersing phase containing the vesicles. Liposomes extemporaneously reconstituted with defibrotide were employed for in vivo experiments in rats. The experimental data presented in this study have shown that positive charge liposomes lyophilized and reconstituted with defibrotide resulted in the formation of complexes characterized by good stability. Morphological and dimensional features of liposomes after lyophilization and reconstitution did not significatively change. In vivo studie