Preparation of transfersomes encapsulating sildenafil aimed for transdermal drug delivery: Plackett-Burman design and characterization
Preparation of transfersomes encapsulating sildenafil aimed for transdermal drug delivery: Plackett-Burman design and characterization
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DOI：
10.3109/08982104.2014.950276
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发表时间：
2015-03-01
影响因子：
4.4
通讯作者：
Ahmed, Tarek A.
中科院分区：
文献类型：
--
作者：
Ahmed, Tarek A.
本工作的目的是利用Plackett-Burman设计研究不同工艺和处方参数对制备西地那非（SD）传递体的影响。考察了药物与磷脂的摩尔比（X1）、磷脂与表面活性剂的摩尔比（X2）、表面活性剂的亲脂平衡（X3）、水化介质的pH值（X4）、水化时间（X5）和水化温度（X6）对药物囊泡尺寸（Y1）和包封率（EE）的影响。制备条件进行了优化，以最大限度地减少囊泡的大小和最大限度地提高EE。制备的传递体也进行了zeta电位测量，形态和理化特性。确定了实现最佳可取性的因素组合。制备优化的制剂，并再次表征其囊泡大小、EE、体外渗透和变形指数。结果表明，X3和X6对Y1有明显影响，而X1和X4对Y2有明显影响。形态学和理化研究证实了传递体的球形和制剂成分的相容性。最佳处方的包封率为97.21%，囊泡粒径为610 nm。载药传递体的体外渗透速率是药物混悬液的5倍以上。变形指数验证了制剂的弹性。可以再次优化显著变量以产生更小的囊泡尺寸，其可以增加SD从经皮递送系统负载的药物优化的传递体的渗透。
The aim of this work was to study the effect of different processing and formulation parameters on the preparation of sildenafil (SD) transfersomes utilizing the Plackett-Burman design. The drug to phospholipid molar ratio (X1), phospholipid to surfactant ratio (X2), hydrophilic-lipophilic balance of the surfactant (X3), hydration medium pH (X4), hydration time (X5) and the temperature of hydration (X6) were investigated to study their effect on the vesicle size (Y1) and entrapment efficiency (EE) of the drug (Y2). The preparation conditions were optimized to minimize the vesicle size and maximize the EE. The prepared transfersomes were also subjected to zeta potential measurements, morphological and physicochemical characterization. The combinations of factors that achieve the optimum desirability were identified. An optimized formulation was prepared and characterized once more for its vesicle size, EE, in vitro permeation and deformability index. The results revealed that both X3 and X6 had a pronounced effect on Y1, while X1 and X4 showed a significant effect on Y2. Morphological and physicochemical study confirmed the transfersomes spherical shape and compatibility of the formulation ingredients. The formulation with optimum desirability showed EE and vesicle size of 97.21% and 610 nm, respectively. In vitro permeation of the drug-loaded transfersome showed more than 5-fold higher permeation rate compared with drug suspension. Deformability index verified elasticity of the preparation. The significant variables could be optimized again to produce smaller vesicle size that could increase SD permeation from transdermal delivery systems loaded drug optimized transfersomes.