Department of Pharmaceutics, College of Pharmaceutical Sciences and Drug Manufacturing, Misr University for Science and Technology, Giza, Egypt.
Department of Dermatology, STD's and Andrology, Faculty of Medicine, Minia University, Al-Minya, Egypt.
Drug Deliv. 2022 Dec;29(1):1100-1111. doi: 10.1080/10717544.2022.2057619.
The current investigation aimed for loading fenticonazole nitrate (FTN), an antifungal agent with low aqueous solubility, into trans-novasomes (TNs) for management of tinea corporis topically. TNs contain Brij as an edge activator besides the components of novasomes (cholesterol, Span 60, and oleic acid) owing to augment the topical delivery of FTN. TNs were fabricated applying ethanol injection method based on D-optimal experiment. TNs were evaluated with regard to entrapment efficiency percent (EE%), particle size (PS), polydispersity index (PDI), and zeta potential (ZP). Further explorations were conducted on the optimum formulation (F7). F7 showed spherical appearance with EE%, PS, PDI, and ZP of 100.00 ± 1.10%, 358.60 ± 10.76 nm, 0.51 ± 0.004, and -30.00 ± 0.80 mV, respectively. The study revealed the ability of the FTN-cholesterol complex to maintain favorable interactions throughout the molecular dynamics simulation (MDS) study. Moreover, growth was inhibited effectively by F7 than by FTN suspension applying 2,3-bis(2-methyloxy-4-nitro-5-sulfophenyl)-2H-tetrazolium-5-carboxanilide (XTT) reduction assay. Furthermore, a clinical appraisal on patients with tinea corporis fungal lesions confirmed the superiority of F7 compared to Miconaz cream in the magnitude of clinical cure of tinea corporis. Thereby, TNs could be considered as promising vesicles for enhancing the antifungal potential of FTN for the topical management of tinea corporis.
本研究旨在将具有低水溶性的抗真菌药硝酸芬替康唑（FTN）载入转诺瓦司（TNs）中，以局部治疗体癣。TNs 除了含有诺瓦司的成分（胆固醇、Span 60 和油酸）外，还含有 Brij 作为边缘活性剂，以增加 FTN 的局部递送。TNs 是通过基于 D-最优实验的乙醇注入法制备的。TNs 的包封效率百分比（EE%）、粒径（PS）、多分散指数（PDI）和 Zeta 电位（ZP）进行了评估。对最佳配方（F7）进行了进一步的研究。F7 表现出球形外观，EE%、PS、PDI 和 ZP 分别为 100.00 ± 1.10%、358.60 ± 10.76nm、0.51 ± 0.004 和-30.00 ± 0.80mV。该研究表明，FTN-胆固醇复合物能够在分子动力学模拟（MDS）研究中保持有利的相互作用。此外，与 FTN 混悬剂相比，F7 通过 2,3-双（2-甲氧基-4-硝基-5-磺苯基）-2H-四唑-5-羧基苯胺（XTT）还原测定，更有效地抑制了真菌的生长。此外，对体癣真菌病变患者的临床评估证实，与咪康唑乳膏相比，F7 在体癣的临床治愈率方面具有优势。因此，TNs 可被视为增强 FTN 抗真菌潜力的有前途的载体，用于体癣的局部治疗。
