Sustained vaginal delivery of in situ gel containing Voriconazole nanostructured lipid carrier: formulation, in vitro and ex vivo evaluation

Abstract

Voriconazole (VOZ) is an antifungal drug having poor aqueous solubility. VOZ nanostructured lipid carrier (VNLC) was prepared by using melt emulsification followed by ultrasonication technique. The VNLCs were optimized by 3² full factorial design using Design-Expert® software. The optimized VNLC had a particle size, zeta potential and entrapment efficiency of 205.8 nm, −27.1 mV and 78.85%, respectively. The optimized VNLC was further loaded in thermosensitive in situ gel. In vitro release studies of VNLC gel showed sustained release of the drug (98.84 ± 1.26%) for up to 24 h. The ex vivo permeation studies showed higher penetration for the VNLC gel as compared to plain VOZ gel. The in vitro antifungal assay showed higher efficacy of VNLC than that of plain VOZ. The HET-CAM test of the VNLC gel showed no irritation and thus was found to be suitable for vaginal administration. Thus, it can be concluded that the developed VNLC gel showed a sustained release pattern with higher drug localization in the vaginal tissue and thus can offer improved treatment of vaginal candidiasis.

Graphical abstract

Keywords:

• Vaginal Candidiasis
• Voriconazole
• nanostructured lipid carrier
• sustained-release
• in situ gel