构建依托泊苷隐形前体脂质体,并考察其在家兔体内的药动学。采用薄膜分散法构建空白隐形脂质体;硫酸铵梯度法包封依托泊苷;结合真空冷冻干燥技术构建依托泊苷隐形前体脂质体。采用凝胶色谱法测定脂质体包封率;透射电镜观察脂质体的形态;电泳光散射技术测定Zeta电位与粒径分布;以市售依托泊苷注射液和普通脂质体为参比制剂,评价其在家兔体内药动学特点。脂质体平均包封率为83.92%±3.65%,粒径为(124.5±26.9)nm,Zeta电位为(-39.50±1.04)mV,家兔单剂量静脉注射1.5 mg/kg依托泊苷制剂后呈二室模型特征,依托泊苷隐形前体脂质体的T_(1/2β)为(19.26±3.16)h,AUC为(26.04±3.53)μg/h/mL;注射液的T_(1/2β)为(0.94±0.21)h,AUC为(0.98±0.26)μg/h/mL;普通脂质体的T_(1/2β)为(7.99±1.36)h,AUC为(11.65±1.70)μg/h/mL。构建的隐形前体脂质体包封率高,且延长了依托泊苷在血液中的循环时间。 Construct etoposide stealth precursor liposomes, and investigate its pharmacokinetics in rabbits. Blank stealth liposomes were prepared by thin-film dispersion method. Etoposide was encapsulated by ammonium sulfate gradient method. Stereosomal liposomes of etoposide were constructed by vacuum freeze-drying technique. The entrapment efficiency of liposomes was determined by gel chromatography. The morphology of liposomes was observed by transmission electron microscopy. The Zeta potential and particle size distribution were determined by electrophoretic light scattering. Commercially available etoposide injection and conventional liposomes were used as reference Preparation, evaluate its pharmacokinetic characteristics in rabbits. The average entrapment efficiency of liposomes was 83.92% ± 3.65%, the diameter was (124.5 ± 26.9) nm and the Zeta potential was (-39.50 ± 1.04) mV. After a single intravenous injection of 1.5 mg / kg etoposide The T_ (1 / 2β) of etoposide stealthy precursor liposomes was (19.26 ± 3.16) h and the AUC was (26.04 ± 3.53) μg / h / mL. The T_1 / The AUC was (0.98 ± 0.26) μg / h / mL for normal liposomes and (7.99 ± 1.36) h for normal liposomes, and the AUC was (11.65 ± 1.70) μg / h / mL. The constructed stealth precursor liposomes have a high entrapment efficiency and prolong the circulating time of etoposide in the blood.