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目的对18α-GL固体脂质纳米粒(18α-GL-SLN)的药动学进行研究。方法在大鼠股静脉和肝脏同时植入探针,尾静脉给药后,同步微透析采样10 h,HPLC测定透析液中18α-GL的浓度,推算血液及肝脏中真实18α-GL药物浓度,拟合药-时曲线,计算药动学参数,并进行统计分析。结果大鼠尾静脉给予18α-GL-SLN和18α-GL后血液和肝脏的主要药动学参数Cmax、AUC0→T(n)、AUCextra和MRT差异均有统计学意义。与18α-GL水溶液相比,18α-GL-SLN的血液Cmax显著降低,肝脏Cmax显著升高,MRT显著延长,AUC显著增高。结论 18α-GL-SLN给药后药物在大鼠肝脏中的浓度显著升高,存留时间显著延长,提示18α-GL-SLN具有显著的肝脏靶向特性。
Objective To study the pharmacokinetics of 18α-GL solid lipid nanoparticles (18α-GL-SLN). Methods The rat femoral vein and liver were implanted with probe at the same time. After the tail vein was administered, microdialysis was performed simultaneously for 10 h. The concentration of 18α-GL in the dialysate was determined by HPLC. The real 18α-GL concentration in blood and liver was estimated. Fold the drug-time curve, calculate pharmacokinetic parameters, and make statistical analysis. Results The main pharmacokinetic parameters Cmax, AUC0 → T (n), AUCextra and MRT in blood and liver after tail vein injection of 18α-GL-SLN and 18α-GL were all statistically significant. The blood Cmax of 18α-GL-SLN was significantly lower than that of 18α-GL aqueous solution, the Cmax of liver was significantly increased, MRT was significantly prolonged, and AUC was significantly increased. Conclusion The concentration of 18α-GL-SLN in rat liver significantly increased and the retention time was significantly prolonged, which indicated that 18α-GL-SLN had significant liver targeting properties.