title: Cationic solid lipid nanoparticles enhance ocular hypotensive effect of melatonin in rabbit.
abstract: The study was aimed at evaluating whether the ocular hypotensive effect of melatonin (MEL) was enhanced by its encapsulation in cationic solid lipid nanoparticles (cSLN), as well as at determining the tolerability of these formulations on the ocular surface. MEL was loaded in cSLN that had already been shown to be suitable for ophthalmic use. The formulations were prepared using Softisan(®) 100 as the main lipid matrix, with the presence of either stearic (SA) or palmitic acid (PA) as lipid modifiers. A fixed positive charge was provided by the addition of a cationic lipid (didecyldimethylammonium bromide). The ocular hypotensive effect was evaluated by measuring the intraocular pressure (IOP) during 24h in albino rabbits. MEL elicited a significant (p<0.01) IOP reduction in rabbit eye. All the formulations tested in vivo demonstrated a good tolerability. The nanocarrier containing SA was the most effective in terms of IOP reduction (maximum IOP reduction: -7 mmHg), and its effect lasted approximately 24h. The experimental data indicate that the new formulations based on cSLN loaded with MEL represent a potent anti-glaucoma treatment with a safe profile, warranting further clinical evaluation of the proposed nanotechnological strategy.
authors.affiliation: NANO-i, Research Center of Ocular Nanotechnology, Department of Drug Sciences, University of Catania, Catania, Italy.
authors.forename: Antonio
authors.initials: A
authors.lastname: Leonardi
authors.affiliation: Department of Clinical and Molecular Biomedicine, Section of Pharmacology and Biochemistry, School of Medicine, University of Catania, Viale A. Doria 6, Catania 95125, Italy. Electronic address: claudio.bucolo@unict.it.
authors.forename: Claudio
authors.initials: C
authors.lastname: Bucolo
authors.affiliation: Department of Clinical and Molecular Biomedicine, Section of Pharmacology and Biochemistry, School of Medicine, University of Catania, Viale A. Doria 6, Catania 95125, Italy.
authors.forename: Filippo
authors.initials: F
authors.lastname: Drago
authors.affiliation: Department of Clinical and Molecular Biomedicine, Section of Pharmacology and Biochemistry, School of Medicine, University of Catania, Viale A. Doria 6, Catania 95125, Italy.
authors.forename: Salvatore
authors.initials: S
authors.lastname: Salomone
authors.affiliation: NANO-i, Research Center of Ocular Nanotechnology, Department of Drug Sciences, University of Catania, Catania, Italy.
authors.forename: Rosario
authors.initials: R
authors.lastname: Pignatello
mesh_terms: D000818:Animals; D065546:Drug Liberation; D007429:Intraocular Pressure / Q000187:drug effects*; D008055:Lipids / Q000737:chemistry; D008297:Male; D008550:Melatonin / Q000008:administration & dosage* / Q000737:chemistry; D053758:Nanoparticles / Q000008:administration & dosage* / Q000737:chemistry; D019308:Palmitic Acid / Q000737:chemistry; D011817:Rabbits; D013229:Stearic Acids / Q000737:chemistry
chemical_list: D008055:Lipids; D013229:Stearic Acids; D019308:Palmitic Acid; C031183:stearic acid; D008550:Melatonin; C000595885:softisan 100
keywords: Eye drops; Glaucoma; Intraocular pressure; Melatonin; Nanoparticles