Formulation of Miconazole-Loaded Chitosan-Carbopol Vesicular Gel: Optimization to In Vitro Characterization, Irritation, and Antifungal Assessment

• Main Authors: Syed Sarim Imam (Author), Sadaf Jamal Gilani (Author), Ameeduzzafar Zafar (Author), May Nasser Bin Jumah (Author), Sultan Alshehri (Author)
• Format: Book
• Published: MDPI AG, 2023-02-01T00:00:00Z.
• Subjects: article
• Online Access: Connect to this object online.

Summary

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 cm²). Compared to MZBSo (86.76 ± 3.7%), MZBSoG2 showed a significantly (<i>p</i> < 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 <i>Candida albicans</i> and <i>Aspergillus niger</i>. 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.

Item Description

10.3390/pharmaceutics15020581
1999-4923