Abstract
AbstractThe influence of one quinolone on the formation and physical stability of phosphatidylcholine (PC) liposomes is described. Based on Photon Correlation Spectroscopy (PCS) measurements, namely mean diameter and polydispersity, the maximum proportion of quinolone which is compatible with liposome morphology and homogeneous population was established in 30% mole of drug in a PC matrix. This lead to a pharmaceutical formulation which includes the additive D-α-tocoferol as antioxidant, glycerol as a co-solvent and phosphatidylcholine-cholesterol (2:1, mole/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.
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