Fishman P H, Peyman G A, Lesar T
Invest Ophthalmol Vis Sci. 1986 Jul;27(7):1103-6.
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.
作者采用免疫荧光测定法，研究了脂质体包裹对白化兔玻璃体内注射庆大霉素后药代动力学的影响。庆大霉素被包裹于磷脂酰胆碱、磷脂酸和α-生育酚的脂质体中。最终的脂质体悬浮液含有庆大霉素，浓度为10mg/ml，95%被包裹。每只兔子的一只眼睛接受玻璃体内注射（每0.1ml含100mg庆大霉素），注射的要么是脂质体包裹的庆大霉素（LEG），要么是磷酸盐缓冲盐水中的庆大霉素（Gs）。平衡透析将玻璃体液样本中的游离药物与包裹药物分离。LEG组的游离药物峰值浓度显著低于Gs组（P<0.01，非配对t检验）。在24、72、120和192小时时，LEG组的游离和总庆大霉素浓度均显著高于Gs组（P<0.05）。与Gs组相比，LEG组总药物的药时曲线下面积增加了两倍，游离药物增加了1.5倍。
