Pharmacokinetics of PEG-PLA-α-asarone Nanoparticles After Nasal and Intravenous Administration

OBJECTIVE To study the pharmacokinetics of polyethylene glycol-polylactic acid-α-asarone nanoparticles (PEG-PLA-α-asarone nanoparticles) after nasal administration compared with intravenous administration in rats. METHODS The rats were used as model. The pharmacokinetics, brain pharmacokinetics and fluorescent labeling method were used to study the distribution of PEG-PLA-α-asarone nanoparticles after nasal administration compared with intravenous administration in rats. RESULTS The results showed that the AUC_(0-∞) in plasma after intravenous and nasal administrations of PEG-PLA-α-asarone nanoparticles were (11 032.4±1 827.1)ng·mL^-1·min and (5 992.9±717.5) ng·mL^-1·min, C_max were (421.9±100.2)ng·mL^-1 and (171.7±26.3)ng·mL^-1, respectively. The absolute bioavailability F was 54.3% after nasal administration of PEG-PLA-α-asarone nanoparticles. The C_max of α-asarone in brain tissue after intravenous and nasal administrations of PEG-PLA-α-asarone nanoparticles were (217.9±29.9)ng·mL^-1 and (334.2±62.7)ng·mL^-1. The values of AUC_brain/AUC_plasma on PEG-PLA-α-asarone nanoparticles after intravenous and nasal administrations were 1.37 and 2.85, respectively. It had statistically significant. The drug brain targeting efficiency and nasal-brain transmission percentage of PEG-PLA-α-asarone nanoparticles after nasal administration were 208.03% and 52.01%, respectively. The result of fluorescent labeling showed that PEG-PLA-α-asarone nanoparticles had stronger brain targeting after nasal administration. CONCLUSION PEG-PLA-α-asarone nanoparticles are suitable for nasal administration for the treatment of brain diseases.