Department of Pharmaceutics, College of Pharmaceutical Sciences and Drug Manufacturing, Misr University for Science and Technology, Giza, Egypt.
College of Pharmaceutical Sciences and Drug Manufacturing, Misr University for Science and Technology, Giza, Egypt.
Drug Deliv. 2020 Dec;27(1):1514-1523. doi: 10.1080/10717544.2020.1837295.
Fenticonazole nitrate (FTN) is a potent antifungal drug adopted in the treatment of vaginal candidiasis. It has inadequate aqueous solubility hence, novel ultra-deformable liposomes 'Terpesomes' (TPs) were developed that might prevail over FTN poor solubility besides TPs might abstain the obstacles of mucus invasion. TPs were assembled by thin-film hydration then optimized by Box Behnken design utilizing terpenes ratio (X), sodium deoxycholate amount (X), and ethanol concentration (X) as independent variable, whereas their impact was inspected for entrapment efficiency (Y), particle size (Y), and polydispersity index (Y). Design Expert was bestowed to select the optimal TP for more studies. The optimal TP had entrapment efficiency of 62.18 ± 1.39%, particle size of 310.00 ± 8.16 nm, polydispersity index of 0.20 ± 0.10, and zeta potential of -10.19 ± 0.2.00 mV. Elasticity results were greater in the optimal TP related to classical bilosomes. Further, permeation illustrated tremendous permeability from the optimal TP correlated to classical bilosomes, and FTN suspension. Besides, assessment displayed significant inhibition effect in rats from FTN-TPs gel compared to FTN gel. The antifungal potency with undermost histopathological variation was detected in rats treated with FTN-TPs gel. Overall, the acquired findings verified the potency of utilizing FTN-TPs gel for treatment of vaginal candidiasis.
硝酸戊脒（FTN）是一种有效的抗真菌药物，用于治疗阴道念珠菌病。它的水溶性不足，因此开发了新型超变形脂质体“Terpesomes”（TPs），除了可以克服 FTN 溶解度差的问题外，TPs 还可以避免粘液入侵的障碍。TPs 通过薄膜水化法组装，然后通过 Box-Behnken 设计进行优化，利用萜烯比（X）、脱氧胆酸钠量（X）和乙醇浓度（X）作为独立变量，考察其对包封效率（Y）、粒径（Y）和多分散指数（Y）的影响。设计专家被赋予选择最佳的 TP 进行更多的研究。最佳的 TP 具有 62.18 ± 1.39%的包封效率、310.00 ± 8.16nm 的粒径、0.20 ± 0.10 的多分散指数和-10.19 ± 0.2.00 mV 的 zeta 电位。与经典的双脂质体相比，最佳 TP 的弹性结果更大。此外，与经典双脂质体和 FTN 混悬剂相比，最佳 TP 的渗透显示出巨大的渗透性。此外，与 FTN 凝胶相比，FTN-TPs 凝胶在大鼠体内的评估显示出显著的抑制作用。在接受 FTN-TPs 凝胶治疗的大鼠中，检测到最低的组织病理学变化的抗真菌效力。总的来说，这些发现证明了使用 FTN-TPs 凝胶治疗阴道念珠菌病的有效性。
