Intravitreal liposome-encapsulated gentamicin in a rabbit model. Prolonged therapeutic levels

The authors investigated the effect of liposome encapsulation on the pharmacokinetics of gentamicin after intravitreal injection in albino rabbits, using immunofluorescent assay. Gentamicin was encapsulated into liposomes of phosphatidylcholine, phosphatidic acid, and alpha-tocopherol. The final liposomal suspension contained gentamicin, 10 mg/ml, 95% encapsulated. One eye of each rabbit received an intravitreal injection (100 mg gentamicin per 0.1 ml) of either liposome-encapsulated gentamicin (LEG) or gentamicin in phosphate-buffered saline (Gs). Equilibrium dialysis separated free from encapsulated drug in vitreous samples. The peak free drug concentration was significantly less (P less than .01, unpaired t-test) with LEG than with Gs. Concentrations of free and total gentamicin were significantly greater (P less than .05) with LEG than with Gs at 24, 72, 120, and 192 hr. LEG gave a twofold increase in area under the drug concentration time curve for total drug, and a 1.5-fold increase for free drug when compared to Gs.