Xiong You-Xiang, Tang Hong-Xia, Ma Rui, Li Fan-Zhu
School of Pharmacy, Zhejiang Chinese Medical University, Hangzhou 311400, China.
Zhongguo Zhong Yao Za Zhi. 2018 Jun;43(12):2531-2536. doi: 10.19540/j.cnki.cjcmm.20180514.007.
In order to optimize the prescription and preparation process of norcantharidin/tetrandrine dual loaded liposomes, the dual drug loaded liposomes were prepared by film dispersion-ultrasonic method using norcantharidin-mesoporous silica nanoparticles（MSN-NCTD）and tetrandrine（Tet）. With particle size and encapsulation efficiency as comprehensive indexes, the influences of phospholipid cholesterol amount, ultrasonic time and ultrasonic power on prescription process were investigated by orthogonal test; the release characteristics of liposomes were investigated by dialysis method. The results indicated that the best prescription process of prepared norcantharidin/tetrandrine dual loaded liposomes was as follows: phospholipid-cholesterol ratio 2.5:1, ultrasonic time 4 min, ultrasonic power 40%; the encapsulation efficiency was 86.62% and 79.19%respectively for NCTD and Tet;liposomes were well-shaped under the transmission microscope, with average particle size of （207.5±3.6） nm, Zeta potential of （1.345±0.173） mV; and the 48 h cumulative release rates of NCTD and Tet were 85.14% and 85.00% respectively. The experiment results proved that the dual drug loaded liposomes prepared by film dispersion-ultrasonic method had uniform particle size, high encapsulation efficiency and sustained release characteristics.
为优化去甲斑蝥素/粉防己碱双载脂质体的处方及制备工艺，采用去甲斑蝥素-介孔二氧化硅纳米粒（MSN-NCTD）与粉防己碱（Tet），通过薄膜分散-超声法制备双药载脂质体。以粒径和包封率为综合指标，采用正交试验考察磷脂胆固醇用量、超声时间和超声功率对处方工艺的影响；采用透析法考察脂质体的释放特性。结果表明，制备去甲斑蝥素/粉防己碱双载脂质体的最佳处方工艺为：磷脂-胆固醇比2.5∶1，超声时间4 min，超声功率40%；NCTD和Tet的包封率分别为86.62%和79.19%；透射电镜下脂质体形态良好，平均粒径为（207.5±3.6）nm，Zeta电位为（1.345±0.173）mV；NCTD和Tet的48 h累积释放率分别为85.14%和85.00%。实验结果证明，采用薄膜分散-超声法制备的双药载脂质体粒径均匀、包封率高、具有缓释特性。
