PDF(Pubmed)
Abstract：
UNASSIGNED: This study aimed to develop a microemulsion (ME)-based skin delivery platform containing sildenafil citrate (SC)-ME and evaluate its in vitro skin permeability.
UNASSIGNED: Accurate MEs were prepared using pseudo-ternary phase diagrams and a full factorial design with three variables at two levels. After the design phase, suitable ratios of oil, water, and a mixture of surfactant (S) and cosurfactant (CS) were selected to prepare various SC-ME formulations. These SC-MEs were analyzed for stability, droplet size, in vitro SC release, skin permeability, and viscosity properties.
UNASSIGNED: The droplet size of the ME samples ranged from 6.24 to 32.65 nm, with viscosities between 114 to 239 cps. Release profiles indicated that 26 to 60% of SC was released from the different SC-MEs within 24 hours. All ME formulations significantly enhanced the permeability coefficient (P) through rat skin. Specifically, the flux (Jss) in SC-ME7 increased by approximately 117 times (Jss = 0.0235 mg/cm2.h) compared to the control sample (0.0002 mg/cm2.h).
UNASSIGNED: The study concluded that the proportions of the water or oil phase and the S/CS mixture in the MEs significantly influenced the physicochemical characteristics and permeation parameters. The selected MEs improved both the permeability coefficient and the rate of permeation through rat skin. The enhanced drug delivery through and into deep skin layers is a key attribute of an ideal dermal ME. These findings suggest that MEs could serve as effective transdermal delivery systems for SC and similar drugs. However, in vivo assays and clinical research are needed to confirm the therapeutic efficacy of MEs.
UNASSIGNED: Accurate MEs were prepared using pseudo-ternary phase diagrams and a full factorial design with three variables at two levels. After the design phase, suitable ratios of oil, water, and a mixture of surfactant (S) and cosurfactant (CS) were selected to prepare various SC-ME formulations. These SC-MEs were analyzed for stability, droplet size, in vitro SC release, skin permeability, and viscosity properties.
UNASSIGNED: The droplet size of the ME samples ranged from 6.24 to 32.65 nm, with viscosities between 114 to 239 cps. Release profiles indicated that 26 to 60% of SC was released from the different SC-MEs within 24 hours. All ME formulations significantly enhanced the permeability coefficient (P) through rat skin. Specifically, the flux (Jss) in SC-ME7 increased by approximately 117 times (Jss = 0.0235 mg/cm2.h) compared to the control sample (0.0002 mg/cm2.h).
UNASSIGNED: The study concluded that the proportions of the water or oil phase and the S/CS mixture in the MEs significantly influenced the physicochemical characteristics and permeation parameters. The selected MEs improved both the permeability coefficient and the rate of permeation through rat skin. The enhanced drug delivery through and into deep skin layers is a key attribute of an ideal dermal ME. These findings suggest that MEs could serve as effective transdermal delivery systems for SC and similar drugs. However, in vivo assays and clinical research are needed to confirm the therapeutic efficacy of MEs.
摘要：
■本研究旨在开发一种基于微乳液（ME）的含有柠檬酸西地那非（SC）-ME的皮肤递送平台，并评估其体外皮肤渗透性。
■使用伪三元相图和具有两个水平的三个变量的全阶乘设计来制备精确的ME。在设计阶段之后,合适的油比例，水,选择表面活性剂(S)和助表面活性剂(CS)的混合物来制备各种SC-ME制剂。分析了这些SC-ME的稳定性，液滴大小,体外SC释放，皮肤渗透性,和粘度特性。
■ME样品的液滴尺寸范围为6.24至32.65nm，粘度在114到239cps之间。释放曲线表明26-60%的SC在24小时内从不同的SC-ME释放。所有ME制剂都显着提高了通过大鼠皮肤的渗透系数（P）。具体来说,SC-ME7中的通量(Jss)增加了约117倍(Jss=0.0235mg/cm2。h)与对照样品(0.0002mg/cm2。h).
■研究得出的结论是，ME中水或油相与S/CS混合物的比例显着影响了物理化学特性和渗透参数。选定的ME改善了渗透系数和通过大鼠皮肤的渗透速率。通过和进入深皮肤层的增强的药物递送是理想的真皮ME的关键属性。这些发现表明，MEs可以作为SC和类似药物的有效透皮给药系统。然而,需要体内试验和临床研究来确认MEs的治疗效果.
■使用伪三元相图和具有两个水平的三个变量的全阶乘设计来制备精确的ME。在设计阶段之后,合适的油比例，水,选择表面活性剂(S)和助表面活性剂(CS)的混合物来制备各种SC-ME制剂。分析了这些SC-ME的稳定性，液滴大小,体外SC释放，皮肤渗透性,和粘度特性。
■ME样品的液滴尺寸范围为6.24至32.65nm，粘度在114到239cps之间。释放曲线表明26-60%的SC在24小时内从不同的SC-ME释放。所有ME制剂都显着提高了通过大鼠皮肤的渗透系数（P）。具体来说,SC-ME7中的通量(Jss)增加了约117倍(Jss=0.0235mg/cm2。h)与对照样品(0.0002mg/cm2。h).
■研究得出的结论是，ME中水或油相与S/CS混合物的比例显着影响了物理化学特性和渗透参数。选定的ME改善了渗透系数和通过大鼠皮肤的渗透速率。通过和进入深皮肤层的增强的药物递送是理想的真皮ME的关键属性。这些发现表明，MEs可以作为SC和类似药物的有效透皮给药系统。然而,需要体内试验和临床研究来确认MEs的治疗效果.
