The Study Of Long-circulating Praziquantel Liposome

To bring into full play praziquantel efficacy of medicine,or to extend the effective blood concentration time,reducing drug consumption,increasing drug treatment index,lower drug toxicity,and changes in administration to avoid the emergence of such purposes.The toxicology pharmacokinetics and clinical treatment of liposomal praziquantel in the animal body were studied,which had the highest encapsulation efficiency and best stability.To optimize the preparing technique and prescription,praziquantel liposomes were prepared by the thin-film hydration and ultrasonic technique to investigate the effect of velocity,organic solvent and vibrated speed of aether on its encapsulation efficiency and stability.The optimized preparing techniques were determined:methanol,chloroform as organic solvent,the optimum prescription preparation of praziquantel liposome were selected with orthogonal design:lecithin:cholesterol=1:20;praziquantel(lecithin+cholesterol)=1:8;PH of PBS is 7.4,organic solvent:PBS=3:1.The results indicated the prepared liposome under the test conditions had the rate(75.54±0.28%) and best stability.The safety evaluation of liposomal praziquantel was conducted by the acute toxicity tests in rats.Sixty KM rats were randomly divided into 4 groups.There levels of liposomal praziquantel e were injected for 4 week in succession and physiological saline was injected as control group.The growth performance,hematological indicators,serum biochemical and histopathological examination were conduced.The results indicated that the LD₅₀ of liposomal praziquantel are higher than the LD₅₀ of praziquantel,and no difference were observed between trailed and control group.The results indicated that toxicity of liposomeal praziquantel was significantly lower than that of convertional praziquantel.The experiment was conducted in rabbit's body to investigate pharmacokinetics about liposomal praziquantel.A dose of 0.5mg/kg liposomeal praziquantel was given to rabbit's and blood samples were collected at different time to measure the drug concentration.The results showed that drug concentration-time curve conformed to one compartment model and its main pharmacokinetical parameters were t_1/2β 15.3408h,CL0.3973 mL/kg,AUG14.5884 h.mg/mL,which indicated the drug effects time had been extended effectively.