title: Application of Box-Behnken design for preparation of levofloxacin-loaded stearic acid solid lipid nanoparticles for ocular delivery: Optimization, in vitro release, ocular tolerance, and antibacterial activity.
abstract: The aim of the present study was to develop and optimize levofloxacin loaded solid lipid nanoparticles for the treatment of conjunctivitis. Box-Behnken experimental design was applied for optimization of solid lipid nanoparticles. The independent variables were stearic acid as lipid (X1), Tween 80 as surfactant (X2) and sodium deoxycholate as co-surfactant (X3) while particle size (Y1) and entrapment efficiency (Y2) were the dependent variables. Further in vitro release and antibacterial activity in vitro were also performed. The optimized formulation of levofloxacin provides particle size of 237.82 nm and showed 78.71% entrapment efficiency and achieved flux 0.2,493 μg/cm(2)/h across excised goat cornea. In vitro release study showed prolonged drug release from the optimized formulation following Korsmeyer-Peppas model. Antimicrobial study revealed that the developed formulation possesses antibacterial activity against Staphylococcus aureus, and Escherichia coli equivalent to marketed eye drops. HET-CAM test demonstrated that optimized formulation was found to be non-irritant and safe for topical ophthalmic use. Our results concluded that solid lipid nanoparticles are an efficient carrier for ocular delivery of levofloxacin and other drugs.
authors.affiliation: Faculty of Pharmacy, Jamia Hamdard (Hamdard University), M.B. Road, New Delhi 110062, India.
authors.forename: Mirza Salman
authors.initials: MS
authors.lastname: Baig
authors.affiliation: Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia. Electronic address: abdulahad20@yahoo.com.
authors.forename: Abdul
authors.initials: A
authors.lastname: Ahad
authors.affiliation: Faculty of Pharmacy, Jamia Hamdard (Hamdard University), M.B. Road, New Delhi 110062, India.
authors.forename: Mohammed
authors.initials: M
authors.lastname: Aslam
authors.affiliation: Glocal School of Pharmacy, Glocal University, Saharanpur, 247121 Uttar Pradesh, India.
authors.forename: Syed Sarim
authors.initials: SS
authors.lastname: Imam
authors.affiliation: Faculty of Pharmacy, Jamia Hamdard (Hamdard University), M.B. Road, New Delhi 110062, India. Electronic address: aqilmalik@yahoo.com.
authors.forename: Mohd
authors.initials: M
authors.lastname: Aqil
authors.affiliation: Faculty of Pharmacy, Jamia Hamdard (Hamdard University), M.B. Road, New Delhi 110062, India.
authors.forename: Asgar
authors.initials: A
authors.lastname: Ali
mesh_terms: D000818:Animals; D000900:Anti-Bacterial Agents / Q000008:administration & dosage*; D002152:Calorimetry, Differential Scanning; D002645:Chickens; D052978:Disk Diffusion Antimicrobial Tests; D004337:Drug Carriers / Q000737:chemistry*; D016503:Drug Delivery Systems; D065546:Drug Liberation; D005123:Eye / Q000187:drug effects / Q000378:metabolism; D064704:Levofloxacin / Q000008:administration & dosage*; D008055:Lipids / Q000737:chemistry*; D053758:Nanoparticles / Q000737:chemistry* / Q000648:ultrastructure; D009883:Ophthalmic Solutions / Q000008:administration & dosage / Q000737:chemistry; D010316:Particle Size; D010539:Permeability; D012995:Solubility; D013229:Stearic Acids / Q000737:chemistry*; D014961:X-Ray Diffraction
chemical_list: D000900:Anti-Bacterial Agents; D004337:Drug Carriers; D008055:Lipids; D009883:Ophthalmic Solutions; D013229:Stearic Acids; C031183:stearic acid; D064704:Levofloxacin
keywords: Antibacterial activity; Box–Behnken design; HET-CAM; Levofloxacin; Ocular drug delivery; Optimization; SLN; Solid lipid nanoparticles