INFLUENCE OF ONE QUINOLONE ON THE FORMATION AND THE PHYSICAL STABILITY OF LIPOSOMES

The influence of one quinolone on the formation and physical stability of phosphatidylcholine (PC) liposomes is described. Based on Photon C orrelation Spectroscopy (PCS) measurements, namely mean diameter and p olydispersity, the maximum proportion of quinolone which is compatible with liposome morphology and homogeneous population was established i n 30 % mole of drug in a PC matrix. This lead to a pharmaceutical form ulation which includes the additive D-alpha-tocoferol as antioxidant, glycerol as a co-solvent and phosphatidylcholine-cholesterol (2:1, mol e/mole) as the formal lipid matrix. Drug encapsualtions between 30-40 % were found. The feasibility of the-method to scale-up this liposome formulation is discussed in terms of PCS, efficiency of encapsulation and preliminary assays in vivo.