Zhang Xin, Tan Rui, Gu Jian, He Li-Li, Fan Li-Na, Nan Xing-Mei
Zhongguo Zhong Yao Za Zhi. 2014 Mar;39(6):1007-10.
Herpetin (HPT) is an active monomer constituent isolated from lignanoid in seeds of Herpetospermum caudigerum. HPT shows inhibitory effects in hepatic injury and HBV-DNA and the replication. In the study, we successfully prepare herpetin liposomes by film dispersion method for the first time. The prescription process was optimized, with the entrapment efficiency as the index. According to the optimized prescription, the mass ratio of HPT: phospholipids: cholesterol was 2.44:78.05: 19.51, the hydration and de-molding process was performed with 0.5% F68 solution at 50 degrees C, and the water-bath ultrasonic time was 20 min. The HPT liposomes prepared by this method showed an average entrapment efficiency of (94.50 +/- 2.15)% and a particle size of (119.2 +/- 10.7) nm, which was consistent with the trial expectations and will lay a solid foundation for the hepatic targeting delivery system in future.
蛇藤素(HPT)是从藏药波棱瓜子中木脂素类成分中分离得到的一种活性单体成分。HPT对肝损伤、乙肝病毒DNA及复制具有抑制作用。本研究首次采用薄膜分散法成功制备了蛇藤素脂质体。以包封率为指标对处方工艺进行优化。根据优化后的处方,HPT:磷脂:胆固醇的质量比为2.44:78.05:19.51,采用0.5% F68溶液在50℃进行水化脱膜,水浴超声时间为20分钟。用该方法制备的HPT脂质体平均包封率为(94.50±2.15)%,粒径为(119.2±10.7)nm,符合试验预期,为今后肝靶向给药系统奠定了坚实基础。