Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, Government College University Faisalabad, Faisalabad 38000, Pakistan.
Department of Pharmacy Practice, Faculty of Pharmaceutical Sciences, Government College University Faisalabad, Faisalabad 38000, Pakistan.
Molecules. 2022 May 4;27(9):2936. doi: 10.3390/molecules27092936.
The occurrence of fungal infections has increased over the past two decades. It is observed that superficial fungal infections are treated by conventional dosage forms, which are incapable of treating deep infections due to the barrier activity possessed by the stratum corneum of the skin. This is why the need for a topical preparation with advanced penetration techniques has arisen. This research aimed to encapsulate fluconazole (FLZ) in a novasome in order to improve the topical delivery. The novasomes were prepared using the ethanol injection technique and characterized for percent entrapment efficiency (EE), particle size (PS), zeta potential (ZP), drug release, Fourier-transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), thermogravimetric analysis (TGA), scanning electron microscopy (SEM) and antifungal activity. The FN7 formulation with 94.45% EE, 110 nm PS and -24 ZP proved to be the best formulation. The FN7 formulation showed a 96% release of FLZ in 8 h. FTIR showed the compatibility of FLZ with excipients and DSC studies confirmed the thermal stability of FLZ in the developed formulation. The FN7 formulation showed superior inhibition of the growth of compared to the FLZ suspension using a resazurin reduction assay, suggesting high efficacy in inhibiting fungal growth.
在过去的二十年中，真菌感染的发生率有所增加。人们观察到，浅表真菌感染采用常规剂型治疗，由于皮肤角质层具有屏障活性，这些常规剂型无法治疗深部感染。这就是为什么需要一种具有先进渗透技术的局部制剂的原因。本研究旨在将氟康唑（FLZ）包封在新星体中，以改善局部传递。新星体是通过乙醇注入技术制备的，并对包封效率（EE）、粒径（PS）、Zeta 电位（ZP）、药物释放、傅里叶变换红外光谱（FTIR）、差示扫描量热法（DSC）、热重分析（TGA）、扫描电子显微镜（SEM）和抗真菌活性进行了表征。具有 94.45% EE、110nm PS 和-24 ZP 的 FN7 制剂被证明是最佳制剂。FN7 制剂在 8 小时内释放了 96%的 FLZ。FTIR 表明 FLZ 与赋形剂具有相容性，DSC 研究证实了 FLZ 在开发制剂中的热稳定性。与 FLZ 混悬剂相比，FN7 制剂在使用 Resazurin 还原测定法时对 的生长表现出更好的抑制作用，表明其在抑制真菌生长方面具有很高的功效。
