去甲斑蝥素/粉防己碱双载药脂质体的制备工艺及体外释放性质考察  

Preparation process of norcantharidin/tetrandrine dual loaded liposomes and their in vitro release characteristics

作　　者：熊友香[1] 汤红霞 马瑞 李范珠[1] XIONG You-xiang;TANG Hong-xia;MA Rui;LI Fan-zhu(School of Pharmacy,Zhejiang Chinese Medical University,Hangzhou 311400,China)

机构地区：[1]浙江中医药大学药学院

出　　处：《中国中药杂志》2018年第12期2531-2536,共6页China Journal of Chinese Materia Medica

基　　金：浙江省中医药科技计划项目(2015ZB038)

摘　　要：为优选去甲斑蝥素/粉防己碱双载药脂质体的处方及制备工艺,该实验以去甲斑蝥素介孔二氧化硅纳米粒（MSNNCTD）及粉防己碱（Tet）为药物,采用薄膜分散-超声法制备双载药脂质体,以粒径和包封率为综合指标,通过正交试验考察磷脂胆固醇用量、超声时间、超声功率对处方工艺的影响;采用透析法考察脂质体的体外释放特性。结果表明制备的去甲斑蝥素/粉防己碱双载药脂质体,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与Tet的包封率分别为86.62%,79.19%;透射显微镜下可见脂质体外形良好,平均粒径（207.5±3.6）nm,Zeta电位（1.345±0.173）m V;NCTD与Tet的48 h累积释放率分别为85.14%,85.00%。实验结果证明薄膜分散-超声法制备双载药脂质体,包封率较高,粒径均匀,具有体外缓释特性。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 in vitro 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 wellshaped under the transmission microscope,with average particle size of（ 207. 5 ± 3. 6） nm,Zeta potential of（ 1. 345 ± 0. 173） m V;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 in vitro sustained release characteristics.

关 键 词：去甲斑蝥素 粉防己碱 双载药脂质体 包封率 体外释放 

分 类 号：R943[医药卫生—药剂学]