Qushawy Mona, Nasr Ali, Abd-Alhaseeb Mohammed, Swidan Shady
Department of Pharmaceutics, Faculty of Pharmacy, Sinai University, Alarish, North Sinai 45511, Egypt.
Department of Pharmaceutics, Faculty of Pharmacy, University of Tabuk, Tabuk 471, Saudi Arabia.
Pharmaceutics. 2018 Feb 23;10(1):26. doi: 10.3390/pharmaceutics10010026.
Miconazole nitrate (MIC) is an antifungal drug used for treatment of superficial fungal infections. However, it has low skin permeability. Hence, the objective of this study was to prepare miconazole nitrate using Transfersomes to overcome the barrier function of the skin. MIC Transfersomes were prepared using a thin lipid film hydration technique. The prepared Transfersomes were evaluated with respect to entrapment efficiency (EE%), particle size, and quantity of in vitro drug released to obtain an optimized formulation. The optimized formulation of MIC Transfersomes was incorporated into a Carbapol 934 gel base which was evaluated in comparison with a marketed product (Daktarin® cream 2%) for drug content, pH, spreadability, viscosity, in vitro permeation, and in vitro and in vivo antifungal activity. The prepared MIC Transfersomes had a high EE% ranging from (67.98 ± 0.66%) to (91.47 ± 1.85%), with small particle sizes ranging from (63.5 ± 0.604 nm) to (84.5 ± 0.684 nm). The in vitro release study suggested that there was an inverse relationship between EE% and in vitro release. The kinetic analysis of all release profiles was found to follow Higuchi's diffusion model. All independent variables had a significant effect on the dependent variables (-values < 0.05). The prepared MIC transfersomal gel showed higher antifungal activity than Daktarin® cream 2%. Therefore, miconazole nitrate in the form of Transfersomes has the ability to penetrate the skin, overcoming the stratum corneum barrier.
硝酸咪康唑（MIC）是一种用于治疗浅表真菌感染的抗真菌药物。然而，它的皮肤渗透性较低。因此，本研究的目的是使用传递体来制备硝酸咪康唑，以克服皮肤的屏障功能。采用薄膜水化技术制备了MIC传递体。对制备的传递体进行包封率（EE%）、粒径和体外药物释放量评估，以获得优化配方。将优化后的MIC传递体配方加入卡波姆934凝胶基质中，并与市售产品（达克宁®乳膏2%）进行药物含量、pH值、铺展性、粘度、体外渗透以及体外和体内抗真菌活性的比较评估。制备的MIC传递体包封率较高，范围为（67.98±0.66%）至（91.47±1.85%），粒径较小，范围为（63.5±0.604 nm）至（84.5±0.684 nm）。体外释放研究表明，包封率与体外释放呈负相关。所有释放曲线的动力学分析均符合Higuchi扩散模型。所有自变量对因变量均有显著影响（-值<0.05）。制备的MIC传递体凝胶显示出比达克宁®乳膏2%更高的抗真菌活性。因此，传递体形式的硝酸咪康唑具有穿透皮肤、克服角质层屏障的能力。
