Pharmacokinetics of α-asarone after intranasal and intravenous administration with PLA-α-asarone nanoparticles.
10.19540/j.cnki.cjcmm.20170307.009
- Author:
Jin LU
1
;
Li-Wei GUO
2
;
Ting-Ming FU
2
;
Guo-Long ZHU
1
;
Zhen-Nan DAI
1
;
Guan-Jun ZHAN
1
;
Li-Li CHEN
3
Author Information
1. Pharmacy of Zhongda Hospital, Southeast University, Nanjing 210009, China.
2. School of pharinacy, Nanjing University of Chinese Medicine, Nanjing 210023, China.
3. Pharmacy of Nanjing Dachang Hospital, Nanjing 210048, China.
- Publication Type:Journal Article
- Keywords:
PLA-α-asarone nanoparticles;
brain targeting;
intranasal;
pharmacokinetic
- From:
China Journal of Chinese Materia Medica
2017;42(12):2366-2372
- CountryChina
- Language:Chinese
-
Abstract:
PLA-α-asarone nanoparticles were prepared by using organic solvent evaporation method, and their in vivo distribution and brain targeting after intranasal administration were studied as compared with intravenous administration. The results showed that brain targeting coefficient of PLA-α-asarone nanoparticles after intranasal and intravenous administration was 1.65 and 1.16 respectively. The absolute bioavailability, brain-targeting efficiency and the percentage of nasal-brain delivery of PLA-α-asarone nanoparticles were 74.2%, 142.24 and 29.83%, respectively after intranasal administration. The results of fluorescence labeling showed that the fluorescent intensity of coumarin-6 in the brain tissue was the highest after intranasal administration of PLA-α-asarone fluorescent nanoparticles, achieving the purpose of brain-targeted drug delivery. The fluorescent intensity of coumarin-6 in liver tissue after intravenous administration of PLA-α-asarone nanoparticles was much higher than that after intranasal administration, indicating that intranasal administration of PLA-α-asarone nanoparticles could decrease drug-induced hepatotoxicity. In addition, the fluorescent intensity of coumarin-6 in lung tissue was weaker after intranasal administration, which solved the shortcomings of intranasal administration of α-asarone dry powder prepared by airflow pulverization method. In vivo studies indicated that PLA-α-asarone nanoparticles after intranasal administration had a stronger brain targeting as compared with intravenous administration.
