The present research work was designed to prepare Azithromycin (AM)-loaded nano lipid carriers (NLs) for ocular delivery. NLs were prepared by the emulsification-homogenization method and further optimized by the Box Behnken design. AM-NLs were optimized using the independent constraints of homogenization speed (A), surfactant concentration (B), and lipid concentration (C) to obtain optimal NLs (AM-NLop). The selected AM-NLop was further converted into a sol-gel system using a mucoadhesive polymer blend of sodium alginate and hydroxyl propyl methyl cellulose (AM-NLopIG). The sol-gel system was further characterized for drug release, permeation, hydration, irritation, histopathology, and antibacterial activity. The prepared NLs showed nano-metric size particles (154.7 ± 7.3 to 352.2 ± 15.8 nm) with high encapsulation efficiency (48.8 ± 1.1 to 80.9 ± 2.9%). AM-NLopIG showed a more prolonged drug release (98.6 ± 4.6% in 24 h) than the eye drop (99.4 ± 5.3% in 3 h). The ex vivo permeation result depicted AM-NLopIG, AM-IG, and eye drop. AM-NLopIG exhibited significant higher AM permeation (60.7 ± 4.1%) than AM-IG (33.46 ± 3.04%) and eye drop (23.3 ± 3.7%). The corneal hydration was found to be 76.45%, which is within the standard limit. The histopathology and HET-CAM results revealed that the prepared formulation is safe for ocular use. The antibacterial study revealed enhanced activity from the AM-NLopIG.
Keywords: HET CAM; NLs; antibacterial; azithromycin; in situ gel; ocular delivery.