Butoconazole nitrate vaginal sponge: Drug release and antifungal efficacy

Abstract

This work aimed to develop an antifungal vaginal sponge loaded with butoconazole nitrate (BN). Sponges were prepared by lyophilization of different polymers (chitosan, gelatin, hydroxyl propyl methylcellulose (HPMC) and carbopol 934) with calcium chloride as crosslinking agent, sodium carboxymethylcellulose as viscosity modifier and different solubilizers. They were characterized regarding morphology, tensile force, elongation percentage, swelling index and their drug release properties. Mucoadhesion force and residence time with cow vaginal mucosa were also determined. The selected formulae were examined using Fourier transform infrared spectroscopy (FT-IR), differential scanning calorimetry (DSC), the scanning electron microscope (SEM), stability and antifungal activity against Candida albicans. Results revealed that all sponges biodegraded completely within 24 h. Chitosan sponges exhibited favorable values and in-vitro drug release. Selected chitosan sponges were stable for three months regarding their physical properties and their release profile. Agar diffusion susceptibility test revealed that chitosan: HPMC (1: 1) with 1.5% w/v Tween 80- sponge was the most effective in term of fungal eradication compared to other sponges and plain drug as well. The results suggested that this mucoadhesive system could be a very promising alternative for other commercially available vaginal antifungal dosage forms, with longer residence time and improved patient compliance.