Pharmacokinetics of econazole nanoparticles eye drops in the rabbit eyes

Abstract

Objective To detect concentration changes in aqueous humor and cornea of econazole nanoparticles (ECZ-NP) eye drops after its application in rabbit eyes and analyze the pharmacokinetics.Methods Japanese White Rabbits were chosen,whose right eye was used as Test group and left eye was used as Control group,0.3％ ECZ nanoparticles eye drops was used as a test drug and 0.3％ ECZ suspension (ECZ-SP) eye drops was used as a control drug.In the single-dose group and in the loading-dose group,the drug was detected using reversed phase high performance liquid chromatography (RP-HPLC).The ECZ concentrations in aqueous humor and cornea of rabbits at different time points were compared.Results ECZ-NP eye drops showed higher drug levels than suspension eye drops,and there were significant differences between two groups (P＜0.01),or the aqueous humor at 5min time point,and for cornea in a single dose,at 5min,15min,30min,45min,60min,90min and 120min time points.In loading-dose group,drug levels were higher than suspension eye drops,and the comparison between the two groups showed significant difference (P＜0.05)for the aqueous humor at 5 min,15 min,30 min,45 min,120 min time points,and for corneas at time points of 5min,15min,30min.Conclusions The concentrations of ECZ in cornea and in aqueous humor are high,and the pharmacokinetic parameters of ECZ-NP eye drops in rabbit eyes can provide experiment basis for its concrete medication scheme. Key words: Econazole; Nanoparticle; Ocular pharmacokinetics; HPLC