Formulation and optimization of terbinafine HCl loaded chitosan/xanthan gum nanoparticles containing gel: Ex-vivo permeation and in-vivo antifungal studies

Superficial fungal infections require a therapeutic concentration of terbinafine HCl (TB) in the targeted skin tissue, hard to achieve after oral administration due to high protein binding. Therefore, the present study aimed to develop a polymeric nanoparticle-loaded gel system for topical terbinafi...

Ausführliche Beschreibung

Gespeichert in:
Bibliographische Detailangaben
Veröffentlicht in:Journal of drug delivery science and technology 2021-12, Vol.66, p.102935, Article 102935
Hauptverfasser: Pervaiz, Fahad, Mushtaq, Rabia, Noreen, Sobia
Format: Artikel
Sprache:eng
Schlagworte:
Online-Zugang:Volltext
Tags: Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
Beschreibung
Zusammenfassung:Superficial fungal infections require a therapeutic concentration of terbinafine HCl (TB) in the targeted skin tissue, hard to achieve after oral administration due to high protein binding. Therefore, the present study aimed to develop a polymeric nanoparticle-loaded gel system for topical terbinafine delivery with maximum drug retention in skin layers. Terbinafine loaded CH/XG nanoparticles produced by polyelectrolyte complexation method followed by incorporation in carbopol gel. All prepared formulations fell in a size range of 194.28–406.67 nm showing a significantly increasing trend by increasing the concentration of the polymer. Entrapment efficiency was amplified (up to 98.44%) by increasing the polymer concentration due to the increase in solution viscosity. Morphological characteristics of formulation revealed particles of round edges. FTIR analysis confirmed the compatibility of ingredients by showing no interaction between the drug and other components. Ex-vivo permeation studies revealed the drug's biphasic release (initial burst release for 2 h and then slow release) with maximum permeation of 13.95%. Percentage retention of the drug was up to 80.5%, which was significantly higher than marketed formulation. In vivo studies revealed that developed formulation provided a rapid and complete removal of the fungal burden compared to control and marketed formulation. [Display omitted] •Novel Terbinafine HCl loaded Chitosan/xanthan gum nanoparticles containing gel have been formulated and optimized.•Fabricated formulations were characterized for topical delivery with maximum drug retention in skin layers.•Antifungal activity of Terbinafine loaded nanoparticles containing gel has been observed in both ex vivo and in vivo models.•This formulation has a better antifungal activity for cutaneous infection as compared to control and marketed formulation.
ISSN:1773-2247
DOI:10.1016/j.jddst.2021.102935