Abstract

Objective: Solid lipid nanoparticles (SLNs) are at the forefront of the rapidly developing field of nanotechnology with several potential applications in drug delivery and research. The aim of this study was to develop and characterize SLNs formulae of Terbinafine HCl (TFH) for topical drug delivery applications.
 Methods: SLNs were prepared using the solvent injection technique. Glyceryl Monostearate (GMS) served as the lipid base. Three stabilizers; Tween 80, Cremophor RH40, and Poloxamer 188, were used. The effect of stabilizer type and concentration, as well as the lipid concentration, were studied, factorial design of 32*21was applied. The prepared SLNs were characterized regarding their particle size, zeta potential, polydispersity index (PDI), entrapment efficiency percent (EE %), and physicochemical stability. The selected formulae were subjected to further investigations such as morphological studies, in vitro release studies, and Infrared (IR) spectroscopy. They were compared with the marketed cream Lamifen® in term of their antifungal activity against Candida albicans.
 Results: Lipid concentration, together with the type and concentration of stabilizer, appeared to be the main cornerstones which affect the formation of SLNs. Smaller particle size was observed when increasing the stabilizer concentration and decreasing the lipid concentration. Higher EE% was observed when increasing both the stabilizer and the lipid concentrations. Formulae (F6, F12 andF19) were selected as the most suitable SLNs with optimum particle size of 480.2±18.89, 458.6±12.45 and 246.7±10.5 nm, respectively as well as the highest EE% of 87.13±0.19, 93.69±0.7 and 95.06±0.25, respectively. In vitro microbiological screening of their antifungal activity showed significantly larger zones of inhibition of diameters 25.9±0.25, 25±0.35 and 24.67±0.36 mm, respectively in comparison with the marketed Lamifen® cream which showed a zone of 11.2±0.44 mm diameter.
 Conclusion: Applying SLNs containing TFH as topical antifungal preparations may be considered as a very promising option as they show good physicochemical characterization with high antifungal activity, which delineates them as a promising dosage form for topical antifungal treatment.

Highlights

  • Nanoparticles (NPs) are colloidal drug carriers that range between 1 to 1000 nanometres in size with a surrounding interfacial layer

  • Particle size was selected to be one of the dependent variables, and the polydispersity index (PDI) value gave an indication for the homogeneity of the preparations

  • The particle size of the prepared solid lipid nanoparticles (SLNs) was significantly affected by changing the stabilizer type as follows, using poloxamer as stabilizer significantly increased the particle size (**p

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Summary

Introduction

Nanoparticles (NPs) are colloidal drug carriers that range between 1 to 1000 nanometres (nm) in size with a surrounding interfacial layer. NPs have many advantages such as low cost of ingredients, ease of preparation as well as being suitable for the preparation of hydrophilic and lipophilic drugs. These particles designed to enhance the solubility of poorly soluble drugs [1,2,3]. Polymeric NPs are colloidal carriers composed of biodegradable macromolecular polymers They increase the therapeutic performance of the poorly soluble drug in any route of administration, but they suffer from toxic degradation of toxic monomers aggregation [4]. They avoid the toxic effect, which may be obtained by the polymers used in the polymeric system [5, 6]

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