Formulation and Evaluation of Nano Lipid Carrier-Based Ocular Gel System: Optimization to Antibacterial Activity
Sadaf Jamal Gilani, May Bin‐Jumah, Ameeduzzafar Zafar, Syed Sarim Imam, Mohd Yasir, Mohammad Khalid, Sultan Alshehri, Mohammed M. Ghuneim, Fatima M. Albohairy
Abstract
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.