Studies On Breviscapine Proliposomes

Breviscapine, a well-known bioactive flavonoid ingredient extracted from Erigeron breviscapus (Vant.) Hand.-Mazz., is mainly composed of scutellarin. Breviscapine possesses potent pharmacological effects in reducing blood viscosity, dilating blood vessel, increasing cerebral blood flow, inhibiting platelet aggregation, improving microcirculation, etc, and are extensively used in clinic to treat ischemic cerebrovascular and cardiovascular diseases in China, such as cerebral infarction, apoplexy, coronary heart disease and angina pectoris, etc.It has been reported that the oral bioavailability of breviscapine is very low and the residence time of breviscapine in the circulation is short. Therefore, the purpose of the article was to increase its bioavailability after oral administration. Breviscapine proliposomes were prepared by spray drying method and fluidized bed method. Study on the stabilities and properties of breviscapine proliposomes prepared by spray method, and more to evaluate the advantage of the preparation of liposomes by the studies on its pharmacokinetics and pharmacodynamics.Ultrafiltration was applied to separate the free breviscapine from the liposomes; The content of scutellarin was determined by HPLC, and the content of breviscapine was determined by UV too. Develop the inverse dialysis method for the liposomes release tests.Seeing about the preparation technics of breviscapine proliposomes. The encapsulation efficiency of proliposomes prepared by fluidized bed method was less then 60 percent, and its technical operation was complicated compared with spray drying method. So we studied on the spray drying method detailed, examine the influences of prescription and technics on encapsulation efficiency by the single factors tests, and the uniform design was used to obtain the optimized prescription. By the spray drying method, the fluidity of the proliposome particles was well, and the encapsulation efficiency was more then 80%. The stabilities of soybean lecithin and breviscapine were well during the spray drying.Some properties of spray-drying breviscapine prolipoaomes were determined. The results showed that the angle of repose of proliposome particles was 38 degree, and the mean particle size of them was 32 μm. The release tests indicated that it was slow when breviscapine was released from liposomal breviscapine. The size distribution of liposomal...