Preparation and Pharmacokinetics in Rats of Voriconazole Long-circulation Liposomes / 中国药师

ABSTRACT

Objective: To prepare voriconazole long-circulation liposomes and evaluate the characteristics of pharmacokinetics in rats.Methods: Voriconazole long-circulation liposomes were prepared by a thin film dispersion extrusion method.The drug release of voriconazole from the long-circulation liposomes was investigated in phosphate buffer solution (PBS) and in rat plasma.The physicochemical properties of the long-circulation liposomes before and after the freeze-drying were studied, such as the particle diameter and the particle shape.The concentration of voriconazole in plasma was determined after tail-vein injection of the long-circulation liposomes in rats.Results: The mean particle size of voriconazole long-circulation liposomes was (192.1±49.3)nm with homogeneous small spherical morphology as seen under a transmission electron microscope.Voriconazole was released in a sustained manner in PBS while much faster in plasma from the long-circulation liposomes.The t1/2 and AUC0-t of the long-circulation liposomes was respectively 2.17 and 2.31 times higher than that of voriconazole injection.Conclusion: Long-circulation liposomes prolong the circulation time and increase the bioavailability of voriconazole.