Jamali Nasibeh, Moghimipour Eskandar, Nikpour Fatemeh, Salimi Anayatollah
Department of Pharmaceutics, Faculty of Pharmacy, Ahvaz Jundishapur University of Medical Sciences, Ahvaz, Iran.
Nanotechnology Research Center, Ahvaz Jundishapur University of Medical Sciences, Ahvaz, Iran.
Iran J Pharm Res. 2024 Mar 28;23(1):e139381. doi: 10.5812/ijpr-139381. eCollection 2024 Jan-Dec.
This study aimed to develop a microemulsion (ME)-based skin delivery platform containing sildenafil citrate (SC)-ME and evaluate its in vitro skin permeability.
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.
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 (J) in SC-ME7 increased by approximately 117 times (J = 0.0235 mg/cm.h) compared to the control sample (0.0002 mg/cm.h).
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.
本研究旨在开发一种基于微乳（ME）的皮肤给药平台，该平台包含枸橼酸西地那非（SC）-ME，并评估其体外皮肤渗透性。
使用伪三元相图和三变量两水平的全因子设计制备精确的微乳。在设计阶段之后，选择合适的油、水以及表面活性剂（S）和助表面活性剂（CS）混合物的比例来制备各种SC-ME制剂。对这些SC-ME进行稳定性、液滴大小、体外SC释放、皮肤渗透性和粘度特性分析。
ME样品的液滴大小范围为6.24至32.65nm，粘度在114至239cps之间。释放曲线表明在24小时内，26%至60%的SC从不同的SC-ME中释放出来。所有ME制剂均显著提高了透过大鼠皮肤的渗透系数（P）。具体而言，与对照样品（0.0002mg/cm·h）相比，SC-ME7中的通量（J）增加了约117倍（J = 0.0235mg/cm·h）。
该研究得出结论，微乳中水相或油相以及S/CS混合物的比例显著影响其物理化学特性和渗透参数。所选微乳提高了透过大鼠皮肤的渗透系数和渗透率。增强药物透过并进入深层皮肤的能力是理想的皮肤微乳的关键特性。这些发现表明微乳可作为SC及类似药物的有效透皮给药系统。然而，需要进行体内试验和临床研究以确认微乳的治疗效果。
