Formulation and in vitro and in vivo evaluation of surfactant-stabilized mucoadhesive nanogels for vaginal delivery of fluconazole

Abstract

Surfactant-stabilized mucoadhesive nanogels (NGs) for vaginal delivery of fluconazole (FLZ) were studied and evaluated in this work. FLZ-NG formulations were prepared using two different types of mucoadhesive polymers, Carbopol 934 (Ca934) and Pluronic F-127 (PF127). A rheology study revealed a non-Newtonian pseudoplastic flow behavior (shear thinning) in the prepared NGs. The viscosity of Ca934 NG (0.47 Pa s) was much lower compared to the PF127 NG (6.10 Pa s). The rheology study results correlated well with the in vitro FLZ release profile from the NG formulations. A pH study (pH = 3.90–4.90) revealed that the formulations were physiologically suitable for vaginal application, to avoid the irritation of the vaginal mucosa. Finally, in vitro and in vivo antimicrobial tests were performed. FLZ incorporated into the Ca934 gel had the strongest antimicrobial effect, with a mean inhibition zone of 24 ± 1.6 mm. Based on these results, it was concluded that the mucoadhesive NG incorporating FLZ resulted in a sustained release and enhanced antimicrobial effect, which would enhance and prolong the therapeutic effects of vaginally delivered FLZ.

Keywords:

• Antifungal activity
• Carbopol 934
• fluconazole
• mucoadhesive nanogel
• Pluronic F-127

Acknowledgement

The authors thank the Deanship of Scientific Research and RSSU at King Saud University for their technical support.

Disclosure statement

Authors report on conflict of interests.

Additional information

Funding

The authors extend their sincere appreciation to the Vice Deanship of Research Chair at King Saud University, Saudi Arabia for funding the work through Kayyali Chair for Pharmaceutical Industries via grant no. MS-2021.