Antibacterial Activity of Contact Lenses Bearing Surface-Immobilized Layers of Intact Liposomes Loaded With Levofloxacin

In vitro methods to evaluate antibacterial activity were used with contact lenses bearing levofloxacin‐loaded liposomes developed for the prevention and treatment of bacterial ocular infections such as keratitis. Levofloxacin was incorporated into liposomes before these intact liposomes were immobilized onto the surfaces of soft contact lenses using a multilayer immobilization strategy. The release of levofloxacin from contact lenses bearing 2, 5, and 10 layers of liposomes into a saline buffer at 37°C was monitored by fluorescence. The levofloxacin release, as a function of time, was described by a mechanism taking into account two independent first‐order kinetic models. The total release of levofloxacin from the contact lenses was completed within 6 days. The release of levofloxacin from contact lenses bearing 10 layers of liposomes and subsequently soaked overnight in a levofloxacin solution was also studied and compare to that of dried contact lenses without any chemical modification rehydrated in a levofloxacin solution. The antibacterial activity of the liposome‐coated contact lenses against Staphylococcus aureus was evaluated by measuring (i) the diameters of the inhibition zone on an agar plate and (ii) the optical density using a broth assay. The liposome‐coated lenses showed an antibacterial activity both on agar and in broth following 24 h. When initial bacteria inocula were equal or below 106 CFU/mL, all the bacteria were inhibited within 2 h. When using initial bacteria inocula of 108 CFU/mL, an initial burst release provided by soaking the liposomal lenses was required for the first hours to inhibit bacteria growth. © 2007 Wiley‐Liss, Inc. and the American Pharmacists Association J Pharm Sci 96: 2350-2363, 2007