Study on pharmacokinetics of novel lung-targeted Docetaxel liposome in in-situ lung cancer model rabbit
- VernacularTitle:新型肺靶向多西他赛脂质体在原位肺癌模型兔中的药动学研究
- Author:
Lijuan WANG
1
;
Rui LI
2
;
Keke CHE
3
;
Yu YU
4
Author Information
1. School of Pharmacy，Chongqing Medical and Pharmaceutical College/Chongqing Engineering Research Center of Pharmaceutical Sciences，Chongqing 401331，China
2. Yaopharma Co.，Ltd.，Chongqing 401121，China
3. Dept. of Pharmacy，Chongqing General Hospital，Chongqing 400014，China
4. College of Pharmacy，Chongqing Medical University，Chongqing 400016，China
- Publication Type:Journal Article
- Keywords:
docetaxel;
liposome;
in-situ lung cancer model;
pharmacokinetics
- From:
China Pharmacy
2023;34(15):1835-1839
- CountryChina
- Language:Chinese
-
Abstract:
OBJECTIVE To study the pharmacokinetic behavior of novel lung-targeted Docetaxel liposome （DTX-LP） in in- situ lung cancer model rabbit. METHODS The content of DTX in rabbit plasma was determined by UPLC-MS/MS， and methodology investigation was conducted. in-situ lung cancer model rabbit was made by the ultra-minimal invasive percutaneous puncture inoculation method. Model rabbits were randomly divided into Docetaxel injection （DTX-IN） group and DTX-LP group. The rabbits were given relevant medicine via ear vein at a dose of 1.0 mg/kg （calculated by DTX）； blood was taken at 5， 15， 30， 60， 90， 120， 240 and 480 minutes to measure the concentration of DTX in plasma. DAS 3.3 software was adopted for fitting and analysis， and to calculate pharmacokinetic parameters. RESULTS UPLC-MS/MS method used in this study was accurate and precise， which met the requirements of biological sample analysis. Compared with DTX-IN group， drug concentration-time curve of DTX-LP was smoother， the blood concentration at each time point was lower， and cmax， t1/2， AUC0→480 min and AUC0→∞ were significantly decreased （P＜0.05）. CONCLUSIONS The drug exposure of DTX-LP in plasma is significantly reduced than DTX- IN， indicating it can be rapidly distributed from systemic circulation to liver target organs.
