Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, October 6 University, Giza, Egypt.
Department of Dermatology, STD's and Andrology, Faculty of Medicine, Minia University, Al-Minya, Egypt.
Int J Nanomedicine. 2021 Jan 8;16:119-132. doi: 10.2147/IJN.S287383. eCollection 2021.
This manuscript aimed at encapsulating an antifungal terconazole (TCZ) into innovative novasomes for improving its penetration into the skin and clinically modulating its therapeutic efficacy.
Novasomes containing free fatty acid (FFA) as a penetration enhancer were formulated using ethanol injection technique based on 2 full factorial design to explore the impact of various formulation variables on novasomes characteristics regarding entrapment efficiency percent (EE%), particle size (PS), polydispersity index (PDI), and zeta potential (ZP). The optimum formulation was chosen using Design-Expert software and utilized for further explorations.
The chosen formulation (N15; including 100 mg lipid components and Span 80 to oleic acid in a ratio of 2:1 (w/w)) exhibited an EE% = 99.45 ± 0.78%, PS = 623.00 ± 2.97 nm, PDI = 0.40 ± 0.04, and ZP = -73.85 ± 0.64 mV. N15 showed spherical vesicles with a higher deformability index (DI) (9.62 ± 0.15 g) compared to traditional niosomal formulation (0.92 ± 0.12 g). Further, N15 showed superior inhibition of growth relative to TCZ suspension using XTT (2,3-bis-(2-methyloxy-4-nitro-5-sulfophenyl)-2H-tetrazolium-5-carboxanilide) reduction assay. Moreover, in vivo skin deposition tests revealed a superior TCZ deposition inside the skin from N15 in comparison to traditional niosomal formulation and TCZ suspension. Furthermore, histopathological examination for rats assured the safety of N15 for topical use. A clinical study conducted on infants suffering from napkin candidiasis proved the superiority of N15 to placebo in providing a complete cure of such fungal infections.
Concisely, the obtained outcomes confirmed the pronounced efficacy of N15 to successfully treat skin fungal infections.
本研究旨在将抗真菌药物替康唑（TCZ）封装于新型的神经酰胺体中，以提高其透皮能力并临床调节其治疗效果。
使用乙醇注入技术，基于 2 因素全析因设计，制备含有游离脂肪酸（FFA）作为渗透增强剂的神经酰胺体，以研究各种制剂变量对神经酰胺体特性（包封效率百分比（EE%）、粒径（PS）、多分散指数（PDI）和 Zeta 电位（ZP））的影响。使用 Design-Expert 软件选择最佳配方，并进行进一步探索。
选择的配方（N15；脂质成分 100mg，与 Span 80 到油酸的比例为 2:1（w/w））表现出 EE%=99.45±0.78%、PS=623.00±2.97nm、PDI=0.40±0.04 和 ZP=-73.85±0.64mV。N15 表现出较高的变形指数（DI）（9.62±0.15g），与传统的神经酰胺体配方（0.92±0.12g）相比，具有更好的变形性。此外，N15 在用 XTT（2,3-双-(2-甲氧基-4-硝基-5-磺苯基)-2H-四唑-5-羧基苯胺）还原测定中显示出对 生长的抑制作用优于 TCZ 混悬液。此外，体内皮肤沉积试验显示，与传统的神经酰胺体配方和 TCZ 混悬液相比，N15 能在皮肤内更好地沉积 TCZ。此外，对大鼠进行的组织病理学检查确保了 N15 用于局部应用的安全性。一项针对患有尿布念珠菌病的婴儿进行的临床研究证明，N15 优于安慰剂，能完全治愈此类真菌感染。
总之，研究结果证实了 N15 成功治疗皮肤真菌感染的显著疗效。
