Department of Pharmaceutics, Seemanta Institute of Pharmaceutical Sciences, Mayurbhanj, Jharpokharia, Odisha, 757086, India.
Department of Pharmaceutics, School of Pharmaceutical Sciences, Siksha 'O' Anusandhan (Deemed to be University), Bhubaneswar, Odisha, 751003, India.
AAPS PharmSciTech. 2023 Nov 21;24(8):240. doi: 10.1208/s12249-023-02698-2.
The objective of the present research was to develop fluconazole-loaded transferosomal bigels for transdermal delivery by employing statistical optimization (2 factorial design-based). Thin-film hydration was employed to prepare fluconazole-loaded transferomal suspensions, which were then incorporated into bigel system. A 2 factorial design was employed where ratios of lipids to edge activators, lipids (soya lecithin to cholesterol), and edge activators (sodium deoxycholate to Tween 80) were factors. Ex vivo permeation flux (Jss) of transferosomal bigels across porcine skin was analyzed as response. The optimal setting for optimized formulation (FO) was A= 4.96, B= 3.82, and C= 2.16. The optimized transferosomes showed 52.38 ± 1.76% DEE, 76.37 nm vesicle size, 0.233 PDI, - 20.3 mV zeta potential, and desirable deformability. TEM of optimized transferosomes exhibited a multilamelar structure. FO bigel's FE-SEM revealed a globule-shaped vesicular structure. Further, the optimized transferosomal suspension was incorporated into thyme oil (0.1% w/w)-containing bigel (TO-FO). Ex vivo transdermal fluconazole permeation from different transferosomal bigels was sustained over 24 h. The highest permeation flux (4.101 μg/cm/h) was estimated for TO-FO bigel. TO-FO bigel presented 1.67-fold more increments of antifungal activity against Candida albicans than FO bigel. The prepared thyme oil (0.1% w/w)-containing transfersomal bigel formulations can be used as topical delivery system to treat candida related fungal infections.
本研究旨在通过采用统计学优化（基于 2 因素设计）开发用于经皮传递的氟康唑负载传递体大凝胶。采用薄膜水化法制备氟康唑负载传递体混悬液，然后将其纳入大凝胶系统。采用 2 因素设计，其中脂质与边缘活性剂的比例、脂质（大豆卵磷脂与胆固醇）和边缘活性剂（脱氧胆酸钠与吐温 80）为因素。作为响应分析了跨猪皮的传递体大凝胶的体外渗透通量（Jss）。优化配方（FO）的最佳设定为 A=4.96、B=3.82 和 C=2.16。优化后的传递体显示出 52.38±1.76%的 DEE、76.37nm 的囊泡大小、0.233 的 PDI、-20.3mV 的 zeta 电位和理想的变形性。优化传递体的 TEM 显示出多层结构。FO 大凝胶的 FE-SEM 显示出球状囊泡结构。此外，将优化的传递体混悬液纳入含有百里香精油（0.1%w/w）的大凝胶（TO-FO）中。不同传递体大凝胶的经皮氟康唑渗透在 24 小时内持续进行。TO-FO 大凝胶的最高渗透通量（4.101μg/cm/h）。TO-FO 大凝胶对白色念珠菌的抗真菌活性增加了 1.67 倍，优于 FO 大凝胶。制备的含有 0.1%w/w 百里香精油的传递体大凝胶制剂可用作局部递送系统来治疗与念珠菌相关的真菌感染。
