Effect of Gelucire 44/14 on Fluconazole Solid Lipid Nanoparticles: Formulation, Optimization and in vitro Characterization

Abstract

Objective: The aim of the present study was to investigate the effect of lauroyl macrogolglycerides (Gelucire 44/14) on Fluconazole (FZ) loaded solid lipid nanoparticles (SLN). Methods: FZ SLN were prepared using Glyceryl monostearate (GMS) and Gelucire 44/14 (GL) by microemulsion technique. The effect of concentration of GL on FZ SLN was studied. Similarly, the effect of formulation variables, drug content in lipid phase (X1) and Surfactant mixture: lipid ratio (X2), on particle size (Y1), entrapment (Y2) and release (Y3) of FZ loaded SLN was also studied using 32 full factorial design. SLN was characterized for particle size, entrapment efficiency, drug content, drug release, morphology by TEM and in-vitro antifungal efficacy. The solid state characterization of optimized lyophilized formulation was performed by DSC and XRD. Results: For the optimized formulation, particle size was 143 nm, PDI 0.38, drug entrapment 75.2% and FZ release after 8 h of dissolution 84.9%. Incorporation of GL in SLN not only decreased the particle size, increased the percent entrapment efficiency and enhanced the drug release but also stabilized the formulation. In-vitro antifungal activity revealed significant reduction in Candida count with FZ SLN [from 4.51 log CFU/ml (T0) to 3.64 log CFU/ml (T24)]. Conclusion: Present study suggests that the developed system might serve as a potential system of drug delivery for Candidiasis. Keywords: Antifungal, Candidiasis, Fluconazole, Gelucire, Mucosal drug delivery, Solid lipid nanoparticles.