关键词: Fenticonazole Nitrate confidence interval and docking study olaminosomes terpesomes

Mesh : Rats Animals Female Drug Delivery Systems / methods Antifungal Agents / pharmacology Administration, Cutaneous Nitrates Rats, Wistar Imidazoles Surface-Active Agents / chemistry Particle Size Drug Carriers

来  源:   DOI:10.1080/10717544.2023.2179129

Abstract:
This review aims to comprehensively highlight the recent nanosystems enclosing Fenticonazole nitrate (FTN) and to compare between them regarding preparation techniques, studied factors and responses. Moreover, the optimum formulae were compared in terms of in vitro, ex vivo and in vivo studies in order to detect the best formula. FTN is a potent antifungal imidazole compound that had been used for treatment of many dangerous fungal infections affecting eye, skin or vagina. FTN had been incorporated in various innovative nanosystems in the recent years in order to achieve significant recovery such as olaminosomes, novasomes, cerosomes, terpesomes and trans-novasomes. These nanosystems were formulated by various techniques (ethanol injection or thin film hydration) utilizing different statistical designs (Box-Behnken, central composite, full factorial and D-optimal). Different factors were studied in each nanosystem regarding its composition as surfactant concentrations, surfactant type, amount of oleic acid, cholesterol, oleylamine, ceramide, sodium deoxycholate, terpene concentration and ethanol concentration. Numerous responses were studied such as percent entrapment efficiency (EE%), particle size (PS), poly-dispersity index (PDI), zeta potential (ZP), and in vitro drug release. Selection of the optimum formula was based on numerical optimization accomplished by Design-Expert® software taking in consideration the largest EE %, ZP (as absolute value) and in vitro drug release and lowest PS and PDI. In vitro comparisons were done employing different techniques such as Transmission electron microscopy, pH determination, effect of gamma sterilization, elasticity evaluation and docking study. In addition to, ex vivo permeation, in vivo irritancy test, histopathological, antifungal activity and Kinetic study.
摘要:
这篇综述旨在全面强调最近的纳米系统包围硝酸芬替康唑(FTN),并在制备技术方面进行比较。研究了因素和对策。此外,在体外比较了最佳配方,离体和体内研究,以检测最佳配方。FTN是一种有效的抗真菌咪唑化合物,已用于治疗许多影响眼睛的危险真菌感染,皮肤或阴道。近年来,FTN已被纳入各种创新的纳米系统中,以实现显着恢复,例如,新生体,cerosomes,子宫体和跨新生体。这些纳米系统是通过各种技术(乙醇注入或薄膜水合)利用不同的统计设计(Box-Behnken,中心复合材料,全阶乘和D-最优)。研究了每个纳米系统中关于其组成作为表面活性剂浓度的不同因素,表面活性剂类型,油酸的量,胆固醇,油胺,神经酰胺,脱氧胆酸钠,萜烯浓度和乙醇浓度。研究了许多反应,如截留效率百分比(EE%),粒度(PS),多分散指数(PDI),zeta电位(ZP),和体外药物释放。最佳配方的选择基于Design-Expert®软件完成的数值优化,并考虑了最大的EE%,ZP(以绝对值表示)与体外药物释放度和最低的PS和PDI。体外比较采用不同的技术,如透射电子显微镜,pH测定,γ灭菌效果,弹性评价与对接研究。此外,离体渗透,体内刺激试验,组织病理学,抗真菌活性和动力学研究。
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