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

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

Volume: 5 Issue: 3

Author(s): Sanjeevani S. Deshkar, Naved A. Quazi, Arun T. Patil and Sushilkumar S. Poddar

Affiliation:

Keywords: Antifungal, Candidiasis, Fluconazole, Gelucire, Mucosal drug delivery, Solid lipid nanoparticles.

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.

Cite this article as:

Deshkar S. Sanjeevani, Quazi A. Naved, Patil T. Arun and Poddar S. Sushilkumar, Effect of Gelucire 44/14 on Fluconazole Solid Lipid Nanoparticles: Formulation, Optimization and in vitro Characterization, Drug Delivery Letters 2015; 5 (3) . https://dx.doi.org/10.2174/221030310503160401121141