<p>Ocular infections remain a significant global health challenge, necessitating advanced drug delivery systems to overcome the limitations of conventional formulations. Ofloxacin (Ofx), a broad-spectrum antibiotic, exhibits restricted ocular bioavailability due to poor corneal permeability and rapid precorneal clearance. This study aimed to develop a niosomal gel formulation to enhance Ofx delivery by improving corneal penetration. Niosomal suspensions were prepared via thin-film hydration using four non-ionic surfactants (Span 60, Span 80, Tween 20, Tween 80) at two drug: surfactant: cholesterol ratios (1:1:1 and 1:2:1). The optimized formulation was selected based on particle size (PS), polydispersity index (PDI), and encapsulation efficiency (EE%). Physicochemical characterization included ATR-FTIR for compatibility, SEM and TEM for morphological analysis, and in vitro release studies. The optimized niosomal suspension was incorporated into gel matrices using varying concentrations of Carbopol-934 and HPMC-K4M. Secondary optimization evaluated ex vivo corneal permeability, in vitro release kinetics, and ocular irritancy (HET-CAM assay). The optimal gel formulation (0.25% Carbopol 934 and 0.5% HPMC K4M) demonstrated sustained drug release, superior corneal permeation, and excellent biocompatibility (cumulative irritation score = 0). Stability studies confirmed the robustness of the developed formulation. These findings highlight the potential of Ofx-loaded niosomal gel as a safe and effective strategy for enhanced ocular delivery, addressing key limitations of conventional eye drops.</p> Graphical Abstract <p></p>

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Enhanced Ocular Delivery of Ofloxacin via Niosomal Gel: In Vitro Characterization and Corneal Permeability Assessment

  • Rideb Chakraborty,
  • Prasanjit Show,
  • Naureen Afrose,
  • Avijit Ruidas,
  • Pratibha Bhowmick,
  • Mithun Bhowmick

摘要

Ocular infections remain a significant global health challenge, necessitating advanced drug delivery systems to overcome the limitations of conventional formulations. Ofloxacin (Ofx), a broad-spectrum antibiotic, exhibits restricted ocular bioavailability due to poor corneal permeability and rapid precorneal clearance. This study aimed to develop a niosomal gel formulation to enhance Ofx delivery by improving corneal penetration. Niosomal suspensions were prepared via thin-film hydration using four non-ionic surfactants (Span 60, Span 80, Tween 20, Tween 80) at two drug: surfactant: cholesterol ratios (1:1:1 and 1:2:1). The optimized formulation was selected based on particle size (PS), polydispersity index (PDI), and encapsulation efficiency (EE%). Physicochemical characterization included ATR-FTIR for compatibility, SEM and TEM for morphological analysis, and in vitro release studies. The optimized niosomal suspension was incorporated into gel matrices using varying concentrations of Carbopol-934 and HPMC-K4M. Secondary optimization evaluated ex vivo corneal permeability, in vitro release kinetics, and ocular irritancy (HET-CAM assay). The optimal gel formulation (0.25% Carbopol 934 and 0.5% HPMC K4M) demonstrated sustained drug release, superior corneal permeation, and excellent biocompatibility (cumulative irritation score = 0). Stability studies confirmed the robustness of the developed formulation. These findings highlight the potential of Ofx-loaded niosomal gel as a safe and effective strategy for enhanced ocular delivery, addressing key limitations of conventional eye drops.

Graphical Abstract