Imam Syed Sarim, Gilani Sadaf Jamal, Zafar Ameeduzzafar, Jumah May Nasser Bin, Alshehri Sultan
Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia.
Department of Basic Health Sciences, Foundation Year of Health Colleges, Princess Nourah Bint Abdulrahman University, Riyadh 11671, Saudi Arabia.
Pharmaceutics. 2023 Feb 8;15(2):581. doi: 10.3390/pharmaceutics15020581.
Miconazole nitrate (MN) is a poorly water-soluble and antifungal drug used for fungal infections. The present research work was designed to develop topical MN-loaded bilosomes (BSs) for the improvement of therapeutic efficacy. MZBSs were prepared by using the thin-film hydration method and further optimized by using the Box-Behnken statistical design (BBD). The optimized miconazole bilosome (MZBSo) showed nano-sized vesicles, a low polydispersity index, a high entrapment efficiency, and zeta potential. Further, MZBSo was incorporated into the gel using carbopol 934P and chitosan polymers. The selected miconazole bilosome gel (MZBSoG2) demonstrated an acceptable pH (6.4 ± 0.1), viscosity (1856 ± 21 cP), and spreadability (6.6 ± 0.2 cm). Compared to MZBSo (86.76 ± 3.7%), MZBSoG2 showed a significantly ( < 0.05) slower drug release (58.54 ± 4.1%). MZBSoG2 was found to be a non-irritant because it achieved a score of zero (standard score) in the HET-CAM test. It also exhibited significant antifungal activity compared to pure MZ against and . The stability study results showed no significant changes after stability testing under accelerated conditions. MZ-loaded gels could serve as effective alternative carriers for improving therapeutic efficacy.
硝酸咪康唑（MN）是一种水溶性差的抗真菌药物，用于治疗真菌感染。本研究旨在开发负载咪康唑的局部双分子层脂质体（BSs），以提高治疗效果。采用薄膜水化法制备了咪康唑双分子层脂质体（MZBSs），并使用Box-Behnken统计设计（BBD）进一步优化。优化后的咪康唑双分子层脂质体（MZBSo）呈现出纳米尺寸的囊泡、低多分散指数、高包封率和zeta电位。此外，使用卡波姆934P和壳聚糖聚合物将MZBSo掺入凝胶中。所选的咪康唑双分子层脂质体凝胶（MZBSoG2）表现出可接受的pH值（6.4±0.1）、粘度（1856±21 cP）和铺展性（6.6±0.2 cm）。与MZBSo（86.76±3.7%）相比，MZBSoG2的药物释放明显较慢（<0.05）（58.54±4.1%）。在HET-CAM试验中，MZBSoG2的得分是零（标准得分），因此被认为无刺激性。与纯咪康唑相比，它对 和 也表现出显著的抗真菌活性。稳定性研究结果表明，在加速条件下进行稳定性测试后没有显著变化。负载咪康唑的凝胶可以作为提高治疗效果的有效替代载体。
