Abu El-Enin Amal Saber Mohammed, Khalifa Maha Khalifa Ahmed, Dawaba Aya Mohammed, Dawaba Hamdy Mohammed
Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy (Girls), Al-Azhar University, Cairo, Egypt.
Department of Pharmaceutics, Faculty of Pharmacy, October University for Modern Sciences and Arts, Cairo, Egypt.
J Adv Pharm Technol Res. 2019 Jan-Mar;10(1):20-26. doi: 10.4103/japtr.JAPTR_332_18.
The aim of this study was to explore the potential of proniosomal gel for topical delivery of fluconazole, an antifungal drug used in fungal infections caused by pathogenic fungi. Fluconazole-loaded proniosomal gels were prepared by the coacervation phase separation method using different nonionic surfactants (spans and tweens). The prepared fluconazole proniosomal gels were evaluated for various parameters such as particle size (PS), drug entrapment efficiency percentage (EE%), and drug release. The experimental results showed that the EE% for the prepared formulae are acceptable (85.14%-97.66%) and they are nanosized (19.8-50.1 nm) and the diffusion from the gels gave the desired sustaining effect. F4, which was prepared from span 60, tween 80 (1:1), and cholesterol showed highest EE% and gave slow release (40.50% ± 1.50% after 6 h), was subjected to zeta potential (ZP) test, transmission electron microscopy as well as microbiological study. The results showed a well-defined spherical vesicle with sharp boundaries with good physical stability of fluconazole within the prepared gel. Moreover, F4 showed an excellent microbiological activity represented by a greater zone of inhibition (5.3 cm) compared to control gel (fluconazole in 2% hydroxy propyl methyl cellulose (HPMC) gel formula) (4.2 cm) and plain gel with no drug (0 cm) against . This study showed the suitability of the proniosomal gel in attaining the desired sustainment effect for topical delivery of fluconazole for the management of fungal infection. The physical stability study showed that there was no significant change in EE%, PS, and ZP of fluconazole proniosomal gel after storage for 6 months.
本研究的目的是探索前体脂质体凝胶用于局部递送氟康唑的潜力，氟康唑是一种用于治疗由致病真菌感染引起的真菌感染的抗真菌药物。采用凝聚相分离法，使用不同的非离子表面活性剂（司盘和吐温）制备了载氟康唑前体脂质体凝胶。对制备的氟康唑前体脂质体凝胶进行了粒径（PS）、药物包封率（EE%）和药物释放等各项参数的评估。实验结果表明，所制备配方的EE%是可接受的（85.14%-97.66%），它们是纳米尺寸的（19.8-50.1nm），并且从凝胶中的扩散产生了所需的缓释效果。由司盘60、吐温80（1:1）和胆固醇制备的F4显示出最高的EE%，并具有缓慢释放（6小时后为40.50%±1.50%），对其进行了zeta电位（ZP）测试、透射电子显微镜以及微生物学研究。结果显示，所制备的凝胶中氟康唑具有明确的球形囊泡，边界清晰，具有良好的物理稳定性。此外，与对照凝胶（2%羟丙基甲基纤维素（HPMC）凝胶配方中的氟康唑）（4.2cm）和无药物的空白凝胶（0cm）相比，F4对……显示出优异的微生物活性，表现为更大的抑菌圈（5.3cm）。本研究表明，前体脂质体凝胶适用于实现氟康唑局部递送所需的缓释效果，以治疗真菌感染。物理稳定性研究表明，氟康唑前体脂质体凝胶在储存6个月后，其EE%、PS和ZP没有显著变化。
