Development, characterization and in vitro-in vivo evaluation of Farnesol loaded niosomal gel for applications in oral candidiasis treatment

Heliyon. 2021 Sep 11;7(9):e07968. doi: 10.1016/j.heliyon.2021.e07968. eCollection 2021 Sep.

Abstract

Objectives: The aim of the study was to formulate and characterize the farnesol loaded niosomes comprising gel formulation and perform their in vitro-in vivo evaluation for applications in the treatment of oral candidiasis infections.

Methods: Various gelling systems were evaluated for their rheological and stability properties. The formulation was statistically optimized using experimental design method (Box-Behnken). Transmission electron microscopy (TEM) and Atomic force microscopy (AFM) were used to observe the niosomal surface morphology. Centrifugation method and dialysis method were used to find out the % entrapment efficiency (%EE) and in-vitro release of Farnesol, respectively. In-vitro antifungal effect and cell biocompatibility of the Farnesol loaded niosomal gel was also performed using Candida albicans (C. albicans) as the model organism and epithelial cell line (SW480) by MTT cytotoxicity assay. In-vivo skin irritation test was performed on rabbit skin.

Key findings: Farnesol loaded niosomes were integrated into polymeric gel solution. The optimized formulation demonstrated acceptable % EE (>80%) and an optimum particle size (168.8 nm) along with a sustained release and a long-term storage stability for up to a period of 6 months. TEM and AFM observations displayed a spherical niosome morphology. Farnesol niosomal gel showed a higher antifungal efficacy, ex-vivo skin permeation and deposition in comparison to plain farnesol solution. The niosomal gel also showed negligible cytotoxicity to normal cells citing biocompatibility and was found to be non-toxic and non-irritant to rabbit skin.

Conclusions: This novel niosome loaded gel-based formulation could make the oral candidiasis healing process more efficient while improving patient compliance. With the optimized methodology used in this work, such formulation approaches can become an efficient, industrially scalable, and cost-effective alternatives to the existing conventional formulations.

Keywords: Atomic Force Microscopy; Candida albicans; Electron microscopy; Farnesol; Gel; Nano carrier; Niosomes.