Abstract

Shubhangi Aher73553* and Munjaji Balasaheb Pitale73552

This study focused on the development and characterization of Fluconazole (FLZ) loaded Nano Lipid Carriers (NLCs) based mucoadhesive gel to increase retention time on applied region to treat Vulvovaginal Candidiasis (VVC). FLZ is administered orally or topically to treat VVC, oral route has a cardiac adverse effect known as FLZ-induced Torsade de pointes. Patients with heart conditions and pregnant women are at risk of receiving orally FLZ, hence topical drug delivery is preferable. Nanostructured lipid carriers were formed in this study using a solvent-diffusion approach followed by high-speed homogenization. For the development of nanostructured lipid carriers Generally Recognized As Safe (GRAS) excipients were selected and optimised such as Compritol-888-ATO, oleic acid and tween-80. NLCs were characterised by particle size, Polydispersity Index (PDI), zeta potential, entrapment efficiency%, total drug content, in vitro release for 8 h and results were found to be 234.6 nm, 0.188, -8.25 mV, 78.99% ± 1.92%, 100.04% ± 0.46% and 84.22% ± 0.94% respectively and also examined for shape and morphology through transmission electron microscopy images. Optimized nanostructured lipid carriers were incorporated in gel by using Carbopol^® 974P as gelling agent and was evaluated for pH, total drug content, spreadability and mucoadhesion which were found to be 4.2, 100.65% ± 1.166%, 7.8 cm ± 3.85 cm and 3534.53 ± 4.71 dyne/cm² respectively. Rheological flow of the gel was found to be pseudoplastic. in vitro drug releases, ex vivo permeation, tissue-deposition and antifungal activity against Candida albicans were all compared to commercial formulation. Hen’s Egg Test-Chorioallantoic Membrane (HET-CAM) assay of gel was performed for irritation and was confirmed that formulation is non-irritant.