Hady Mayssa Abdel, Darwish Asmaa B, Abdel-Aziz Mohamed S, Sayed Ossama M
Department of Pharmaceutical Technology, National Research Centre, El Bohouth Street, Cairo12622, Egypt.
Department of Pharmaceutical Technology, National Research Centre, El Bohouth Street, Cairo12622, Egypt.
Colloids Surf B Biointerfaces. 2022 Mar;211:112304. doi: 10.1016/j.colsurfb.2021.112304. Epub 2021 Dec 23.
The objective of this study was to prepare and evaluate Nystatin (NYS) loaded transfersomes to achieve better treatment of vulvovaginal candidiasis. Nystatin transferosomes were formulated utilizing thin film hydration method. A 3 full factorial design was employed to evaluate the effect of different formulation variables. Two independent variables were chosen; the ratio between lecithin surfactant (X) was set at three levels (10-40), and the type of surfactants (X) was set at three levels (Span 60, Span 85 and Pluronic F-127). The dependent responses were; entrapment efficiency (Y: EE %), vesicles size (Y: VS) and release rate (Y: RR). Design Expert® software was utilized to statistically optimize formulation variables. The vesicles revealed high NYS encapsulation efficiency ranging from 97.35 ± 0.03 to 98.01 ± 0.20% whereas vesicle size ranged from 194.8 ± 20.42 to 400.8 ± 42.09 nm. High negative zeta potential values indicated good stability of the prepared formulations. NYS release from transfersomes was biphasic and the release pattern followed Higuchi's model. The optimized formulation (F7) exhibited spherical morphology under transmission electron microscopy (TEM). In-vitro and in-vivo antifungal efficiency studies revealed that the optimized formula F7 exhibited significant eradication of candida infestation in comparison to free NYS. The results revealed that the developed NYS transfersomes could be a promising drug delivery system to enhance antifungal efficacy of NYS.
本研究的目的是制备并评估负载制霉菌素（NYS）的传递体，以更好地治疗外阴阴道念珠菌病。采用薄膜水化法制备制霉菌素传递体。采用三因素全因子设计来评估不同制剂变量的影响。选择了两个自变量；卵磷脂表面活性剂的比例（X）设置为三个水平（10 - 40），表面活性剂的类型（X）设置为三个水平（司盘60、司盘85和普朗尼克F - 127）。因变量响应为；包封率（Y：EE%）、囊泡大小（Y：VS）和释放速率（Y：RR）。利用Design Expert®软件对制剂变量进行统计优化。囊泡显示出较高的制霉菌素包封效率，范围为97.35±0.03%至98.01±0.20%，而囊泡大小范围为194.8±20.42至400.8±42.09纳米。高的负zeta电位值表明所制备制剂具有良好的稳定性。制霉菌素从传递体中的释放是双相的，释放模式遵循Higuchi模型。优化后的制剂（F7）在透射电子显微镜（TEM）下呈现球形形态。体外和体内抗真菌效率研究表明，与游离制霉菌素相比，优化后的配方F7对念珠菌感染有显著的根除作用。结果表明，所开发的制霉菌素传递体可能是一种有前景的药物递送系统，可提高制霉菌素的抗真菌疗效。
