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

Drug Dev Ind Pharm. 2021 Dec;47(12):1935-1942. doi: 10.1080/03639045.2022.2070760. Epub 2022 May 10.

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; Pluronic F-127; fluconazole; mucoadhesive nanogel.

MeSH terms

  • Antifungal Agents / pharmacology
  • Delivery, Obstetric
  • Excipients
  • Female
  • Fluconazole* / pharmacology
  • Gels
  • Humans
  • Nanogels
  • Poloxamer
  • Pregnancy
  • Surface-Active Agents*

Substances

  • Antifungal Agents
  • Excipients
  • Gels
  • Nanogels
  • Surface-Active Agents
  • Poloxamer
  • Fluconazole