阿苯达唑纳米脂质体冻干粉在大鼠体内药动学及肝靶向研究

目的：研究阿苯达唑纳米脂质体冻干粉在大鼠体内的药动学过程及肝脏靶向性。方法：大鼠以灌胃给予阿苯达唑片、阿苯达唑脂质体及阿苯达唑纳米脂质体冻干粉，分别于给药后不同时间点取血及肝脏，样品预处理后利用高效液相色谱（HPLC）法测定血浆及肝组织中药物浓度，考察3种制剂的药动学参数及肝靶向性差异。结果：阿苯达唑纳米脂质体冻干粉主要药动学参数如下：C_max为（7.05±0.70）μg·mL^-1，t_max为（6.15±0.66） h，AUC_0-∞为（150.9±12.1）μg·mL^-1·h，以阿苯达唑片、阿苯达唑脂质体为参比制剂，阿苯达唑纳米脂质体冻干粉相对生物利用度分别为236.04%和178.45%；肝靶向试验结果显示：阿苯达唑纳米脂质体冻干粉在肝组织中的分布显著高于阿苯达唑片和阿苯达唑脂质体。结论：将阿苯达唑脂质体制成纳米级脂质体冻干粉后，可显著提高药物的相对生物利用度和肝靶向性。

Pharmacokinetics and liver targeting of lyophilized albendazole nanoliposomes in rats

OBJECTIVE To research the phamacokinetics and liver targeting of lyophilized albendazole nanoliposomes (NL-ABZ) in rats.METHODS After rats were orally administrated abendazole tablets (T-ABZ),albendazole liposomes (L-ABZ) and lyophilized albendazole nanoliposomes (NL-ABZ),blood and liver samples were collected at different time points.The samples were pretreated and analyzed by high performance liquid chromatography (HPLC) system,and then the differences of phamacokinetics parameters and liver targeting were analyzed.RESULTS Pharmacokinetics of lyophilized NL-ABZ:C_max was (7.05±0.70) μg·mL^-1,t_max was (6.15±0.66) h,AUC_0-∞ was (150.9±12.1) μg·mL^-1·h.Compared with T-ABZ and L-ABZ,relative bioavailabilities of lyophilized NL-ABZ were 236.04% and 178.45%,respectively,and liver had obviously increased distribution of lyophilized albendazole nanoliposomes.CONCLUSION The lyophilized NL-ABZ can improve bioavailability and liver targeting significantly.