Formulation and Evaluation of Nano Lipid Carrier-Based Ocular Gel System: Optimization to Antibacterial Activity

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.

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About this article: Gilani, S.J.; Jumah, M.N.b.; Zafar, A.; Imam, S.S.; Yasir, M.; Khalid, M.; Alshehri, S.; Ghuneim, M.M.; Albohairy, F.M. Formulation and Evaluation of Nano Lipid Carrier-Based Ocular Gel System: Optimization to Antibacterial Activity. Gels 2022, 8, 255. https://doi.org/10.3390/gels8050255

Materials
Azithromycin (AM) was procured from Alembic Pharmaceutical Ltd. (Ahmedabad, India). Glyceryl behenate (GB, melting point ~70 °C), Labrasol, and Precirol ATO-5 were procured from Gattifosse (Mumbai, India). Tripalmitins, Stearic acid, Myristic acid, Glycerol monostearate, Glyceryl monooleate, methanol, and acetonitrile were procured from Sigma-Aldrich (St. Louis, MO, USA). Isopropyl myristate, Miglyol, Coconut oil, Sunflower oil, Labrasol, and Sesame oil were procured from Loba Chemie (Mumbai, India). The Span 60, Span 20, Kolliphor EL, and Cremophor RH60 were procured from Acros organic (Somerset, NJ, USA). Zaha eye drops (Azithromycin eye solution, 1% w/v, Ajanta Pharma, India) were purchased from a local pharmacy.