Alkhalidi Hala M, Hosny Khaled M, Rizg Waleed Y
Department of Clinical Pharmacy, Faculty of Pharmacy, King Abdulaziz University, Jeddah 21589, Saudi Arabia.
Department of Pharmaceutics, Faculty of Pharmacy, King Abdulaziz University, Jeddah 21589, Saudi Arabia.
Pharmaceutics. 2020 Dec 25;13(1):27. doi: 10.3390/pharmaceutics13010027.
Candidiasis is one of the frequently encountered opportunistic infections in the oral cavity and can be found in acute and chronic presentations. The study aimed to develop fluconazole-loaded sesame oil containing nanotransfersomes (FS-NTF) by the thin-layer evaporation technique to improve the local treatment of oral candidiasis. Optimization of the formulation was performed using the Box‒Behnken statistical design to determine the variable parameters that influence the vesicle size, entrapment efficiency, zone of inhibition, and ulcer index. Finally, the formulated FS-NTF was embedded within the hyaluronic acid‒based hydrogel (HA-FS-NTF). The rheological behavior of the optimized HA-FS-NTF was assessed and the thixotropic behavior with the pseudoplastic flow was recorded; this is desirable for an oral application. An in vitro release study revealed the rapid release of fluconazole from the HA-FS-NTF. This was significantly higher when compared with the fluconazole suspension and hyaluronic acid hydrogel containing fluconazole. Correspondingly, the ex vivo permeation was also found to be higher in HA-FS-NTF in sheep buccal mucosa (400 μg/cm) when compared with the fluconazole suspension (122 μg/cm) and hyaluronic acid hydrogel (294 μg/cm). The optimized formulation had an inhibition zone of 14.33 ± 0.76 mm and enhanced antifungal efficacy for the ulcer index (0.67 ± 0.29) in immunocompromised animals with infection; these findings were superior to those of other tested formulations. Hence, it can be summarized that fluconazole can effectively be delivered for the treatment of oral candidiasis when it is entrapped in a nanotransfersome carrier and embedded into cross-linked hyaluronic acid hydrogel.
念珠菌病是口腔中常见的机会性感染之一，可表现为急性和慢性。本研究旨在通过薄膜蒸发技术制备负载氟康唑的芝麻油纳米传递体（FS-NTF），以改善口腔念珠菌病的局部治疗。采用Box-Behnken统计设计对制剂进行优化，以确定影响囊泡大小、包封率、抑菌圈和溃疡指数的可变参数。最后，将制备的FS-NTF包埋于透明质酸基水凝胶（HA-FS-NTF）中。评估了优化后的HA-FS-NTF的流变学行为，并记录了其假塑性流动的触变性行为；这对于口腔应用是理想的。体外释放研究表明氟康唑从HA-FS-NTF中快速释放。与氟康唑混悬液和含氟康唑的透明质酸水凝胶相比，释放量显著更高。相应地，在绵羊颊黏膜中，HA-FS-NTF的离体渗透也高于氟康唑混悬液（122μg/cm）和透明质酸水凝胶（294μg/cm）（400μg/cm）。优化后的制剂在免疫受损感染动物中的抑菌圈为14.33±0.76mm，溃疡指数的抗真菌疗效增强（0.67±0.29）；这些结果优于其他测试制剂。因此，可以总结出氟康唑包裹在纳米传递体载体中并包埋于交联透明质酸水凝胶中时，可有效用于治疗口腔念珠菌病。
