OBJECTIVETo prepare eye drops of puerarin liposomes and investigate its lacrimal pharmacokinetics in rabbit tears.

METHODPuerarin liposomes were prepared by reverse phase evaporation technique. The liposomes and free puerarin were separated by SephadexG-50 chromatography and then encapsulation ratio of liposomes was determined in detail. Micromorphology of liposome particles was observed by electronic transmission microscope and the size distribution of the liposomes was analyzed by laser particle size analyzer. The concentration of puerarin in rabbit's tears was determined by HPLC after ocular administration of 50 microL puerarin liposomes while puerarin eye drops was chosen as control with the same puerarin concentration. The pharmacokinetic parameters were calculated by software program 3P97 according to one-compartment mode.

RESULTGlobal liposome nanoparticles with diameter of about 195.7 nm were prepared successfully. The encapsulation ratio of puerarin in the liposomes was 48.3%. The mean residence time (MRT) value and the area under concentration (AUC) of puerarin in liposome were 3.89 and 3.06 times more than those of puerarin eye drops.

CONCLUSIONLiposomes as a drug carrier can greatly increase the concentration of puerarin in tears, enhance the pre-ocular retention time than that of eye drops.

Animals ; Chromatography, High Pressure Liquid ; Isoflavones ; chemistry ; pharmacokinetics ; Liposomes ; chemistry ; pharmacokinetics ; ultrastructure ; Microscopy, Electron, Transmission ; Ophthalmic Solutions ; chemistry ; pharmacokinetics ; Rabbits ; Tears ; chemistry