白花丹醌传递体凝胶的制备及其体外透皮研究  

Preparation of plumbagin transfersomal gel and investigation on its transdermal penetration characteristics in vitro

作　　者：马闪闪 张志锋 吕露阳 张吉仲 MA Shan-shan;ZHANG Zhi-feng;LV Lu-yang;ZHANG Ji-zhong(School of Pharmacy,Southwest Minzu University,Chengdu 610041,China)

机构地区：[1]西南民族大学药学院,四川成都610041

出　　处：《中草药》2018年第15期3625-3631,共7页Chinese Traditional and Herbal Drugs

基　　金：四川省科技厅应用基础项目(2015YJ0226);中央高校基本科研业务费专项基金项目(2016NGJPY11)

摘　　要：目的制备白花丹醌传递体(PBG-T)凝胶,考察其经皮给药的渗透特性。方法采用薄膜-超声分散法制备PBG-T,通过星点设计-效应面法优化PBG-T处方,通过正交试验优化PBG-T凝胶的处方;垂直式Franz扩散池考察PBG-T凝胶体外透皮扩散效果。结果 PBG-T的最优处方工艺为白花丹醌(PBG)10.0 mg,磷脂700.0 mg,聚山梨酯-80 91.5 mg,超声时间13 min;PBG-T凝胶的最优处方为卡波姆1%,甘油5%;以最优处方制得的PBG-T的包封率为(79.88±2.26)%,平均粒径为(125.64±4.54)nm,Zeta电位为(-30.97±1.13)m V;PBG-T凝胶12 h的累积渗透率为70.0%。结论 PBG-T凝胶的处方工艺稳定、可行,且可以减缓PBG的体外释放,增加其累积渗透率。Objective To prepare plumbagin transfersomal（PBG-T） gel and investigate its transdermal penetration characteristics in vitro. Methods Plumbagin transfersomes were prepared by film-ultrasonic dispersion method. The optimal prescription condition of PBG-T was selected by central composite design and response surface method. The formula of PBG-T gel was optimized by orthogonal test. The Franz diffusion cell was used to investigate transdermal penetration characteristics of PBG-T gel in vitro. Results The optimal prescription condition of transfersomes was determined as drug 10.0 mg, phospholipids 700.0 mg, Tween-80 91.5 mg, ultrasonication time 13 min. The optimal prescription condition of transfersomal gel was 1% carbomer 940 as gel matrix, and 5% glycerol as the humectant. According to the optimized prescription, the entrapment efficiency, the mean particle size, and Zeta potential of PBG-T were（79.88 ± 2.26）%,（125.64 ± 4.54） nm, and（-30.97 ± 1.13） m V. The cumulative penetration rate of PBG-T gel was 70.0% at 12 h. Conclusion The optimal preparation technique is stable and feasible. Transfersomal gel features a sustained release in vitro, the transfersomal gel can increase penetration rate of plumbagin through the skin of rats.

关 键 词：白花丹醌 星点设计-效应面法 传递体 凝胶 透皮给药 正交试验 薄膜-超声分散法 

分 类 号：R283.6[医药卫生—中药学]