[关键词]
[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)mV;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。
[Key word]
[Abstract]
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) mV. 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.
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[基金项目]
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)