<p>This study aimed to develop a nanostructured lipid carrier (NLC) gel for enhanced topical delivery of voriconazole, a primary antifungal agent. Two NLC formulations were prepared using stearic acid, glyceryl monostearate (GMS), and oleic acid as lipid components, utilizing melt dispersion and homogenization techniques. Key properties, including particle size, entrapment efficiency, viscosity, pH, release characteristics, and skin irritation potential, were evaluated to optimize the formulations. Voriconazole-loaded NLCs were formulated with stearic acid, GMS, oleic acid, carbopol 234, Tween 80, hydrogen peroxide, and sodium lauryl sulfate (SLS). Characterization included particle size, zeta potential, entrapment efficiency, optical microscopy, X-ray diffraction (XRD), and ex vivo permeation studies to assess drug release and skin permeation potential. The optimized formulation, NLC2, achieved a particle size of 329&#xa0;nm, a zeta potential of − 23.86&#xa0;mV, and an entrapment efficiency of 91.23%, while NLC1 and NLC2 particle sizes were 692.5&#xa0;nm and 329.9&#xa0;nm, respectively. The formulations showed thixotropic viscosity behavior and pH values of 7.2 to 7.4, suitable for topical application. Drug release studies demonstrated an initial burst followed by sustained release, with NLCF1 achieving 98% drug release through a dialysis membrane and 88% through chicken skin. XRD analysis confirmed the crystalline nature of voriconazole, and spreadability values for NLC formulations were 16.1 ± 0.3 (NLCF1) and 6.5 ± 0.5 (NLCF2). The developed voriconazole-loaded NLC hydrogel demonstrates promising potential for sustained topical drug delivery, with favorable release characteristics and skin compatibility.</p>

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Development and Characterization of Voriconazole-loaded Nanostructured Lipid Carriers for Enhanced Topical Antifungal Therapy

  • Manmayee Mohapatra,
  • Debasis Pradhan,
  • Snehamayee Mohapatra,
  • Rajat Kumar Kar,
  • Goutam Kumar Jena

摘要

This study aimed to develop a nanostructured lipid carrier (NLC) gel for enhanced topical delivery of voriconazole, a primary antifungal agent. Two NLC formulations were prepared using stearic acid, glyceryl monostearate (GMS), and oleic acid as lipid components, utilizing melt dispersion and homogenization techniques. Key properties, including particle size, entrapment efficiency, viscosity, pH, release characteristics, and skin irritation potential, were evaluated to optimize the formulations. Voriconazole-loaded NLCs were formulated with stearic acid, GMS, oleic acid, carbopol 234, Tween 80, hydrogen peroxide, and sodium lauryl sulfate (SLS). Characterization included particle size, zeta potential, entrapment efficiency, optical microscopy, X-ray diffraction (XRD), and ex vivo permeation studies to assess drug release and skin permeation potential. The optimized formulation, NLC2, achieved a particle size of 329 nm, a zeta potential of − 23.86 mV, and an entrapment efficiency of 91.23%, while NLC1 and NLC2 particle sizes were 692.5 nm and 329.9 nm, respectively. The formulations showed thixotropic viscosity behavior and pH values of 7.2 to 7.4, suitable for topical application. Drug release studies demonstrated an initial burst followed by sustained release, with NLCF1 achieving 98% drug release through a dialysis membrane and 88% through chicken skin. XRD analysis confirmed the crystalline nature of voriconazole, and spreadability values for NLC formulations were 16.1 ± 0.3 (NLCF1) and 6.5 ± 0.5 (NLCF2). The developed voriconazole-loaded NLC hydrogel demonstrates promising potential for sustained topical drug delivery, with favorable release characteristics and skin compatibility.