Besifloxacin-loaded ocular nanoemulsions: design, formulation and efficacy evaluation.

Abstract

The purpose of this study was to develop and evaluate nanoemulsions (NEs) containing besifloxacin for ocular drug delivery. Pseudo ternary phase diagrams were constructed using Triacetin (oil), Cremophor® RH 40 (surfactant), and Transcutol®P (co-surfactant) to identify NE regions. Six formulations were developed by low-energy emulsification method and then evaluated for size, refractive index, pH, osmolality, viscosity, anddrug release.After accelerated physical stability and bovine conrneal permeation studies,NE2 was chosen as optimized formulationforantimicrobial efficacy, and hen's egg test-chorioallantoic membrane (HET-CAM)tests. The particle size of optimum NE was 14nm with a narrow size distribution. Moreover, other physicochemical characterizations were in the acceptable range for ocular administration. Besifloxacin-loaded NEs demonstrated sustained release pattern and 1.7-fold higher permeation compared with the control suspension in the ex vivo transcorneal permeation study. HET-CAM test indicated no irritation, and HL% revealed no damage to the tissue, so the optimum NE is well tolerated by the eye. In vitro antimicrobial evaluation, showed comparative efficacy of lower drug-loaded NE (0.2%) versus 0.6% besifloxacin suspension (equal concentration to commercial besifloxacin eye drop). In conclusion, besifloxacin-loaded NEs could be considered as a suitable alternative to the marketed suspension for treatingbacterial eyeinfections.