Study on the tissue distribution and pharmacokinetics of PELGE-crebanine nanoparticles in rats
- VernacularTitle:PELGE-克班宁纳米粒在大鼠体内的组织分布及药动学研究
- Author:
Lili CUI
1
,
2
;
Shujun KONG
3
;
Hui WANG
1
;
Qiuyan HUANG
1
;
Hongmei WANG
1
;
Yunshu MA
1
,
4
Author Information
1. College of Chinese Material Medica，Yunnan University of Chinese Medicine，Kunming 650500，China
2. School of Pharmacy，Nanjing University of Chinese Medicine，Nanjing 210023，China
3. Disha Pharmaceutical Group Co. Ltd.，Shandong Weihai 264200，China
4. Yunnan Key Laboratory of External Drug Delivery System and Preparation Technology in Universities，Kunming 650500，China
- Publication Type:Journal Article
- Keywords:
polyethylene glycol-（polylactic acid-hydroxyacetic
- From:
China Pharmacy
2022;33(24):2957-2961
- CountryChina
- Language:Chinese
-
Abstract:
OBJECTIVE To study the tissue distribution and pharmacokinetic characteristics of polyethylene glycol-（polylactic acid-hydroxyacetic acid） -polyethylene glycol triblock copolymer （PELGE） -crebanine nanoparticles （PELGE-Cre-NPS） in rats. METHODS The SD rats were divided into 9 groups （1 group at each time point）， with 6 rats in each group，half male and half female. After PELGE-Cre-NPs（5 mg/kg） was injected into tail vein of rats， appropriate amounts of heart， liver， spleen， lung， kidney and brain tissues were taken at 5， 15， 30， 60， 90， 120， 180， 240 and 300 min， respectively. With verapamil hydrochloride as internal standard， the content of crebanine （Cre） in each tissue was determined by HPLC， and the main pharmacokinetic parameters such as area under the drug-time curve （AUC0－）t and mean retention time （MRT0－）t were calculated.RESULTS At 5-90 min after medication， the content of Cre in each tissue of rats from large to small was lung， kidney， spleen， liver， brain and heart； at 120-300 min after medication， the sequence was lung， spleen， kidney， liver， brain and heart. AUC0－t of Cre in heart， liver， spleen， lung， kidney and brain were （18.86±1.66）， （43.36±4.99）， （51.36±5.34）， （81.86±12.34）， （53.31±3.19） and （27.73±4.76） mg·h/L， respectively. MRT0－t of Cre were （1.94±0.12）， （1.97±1.02）， （1.98±1.23）， （1.89±0.21）， （1.88± 0.06）， （1.85±0.19） h， respectively. CONCLUSIONS PELGE-Cre-NPs mainly distribute in lung tissue， but less in heart tissue， and the elimination of PELGE-Cre-NPs in heart， lung and liver tissue is slow.
