title: Nanoemulsion as a potential ophthalmic delivery system for dorzolamide hydrochloride.
abstract: Dilutable nanoemulsions are potent drug delivery vehicles for ophthalmic use due to their numerous advantages as sustained effect and high ability of drug penetration into the deeper layers of the ocular structure and the aqueous humor. The aim of this article was to formulate the antiglaucoma drug dorzolamide hydrochloride as ocular nanoemulsion of high therapeutic efficacy and prolonged effect. Thirty-six systems consisting of different oils, surfactants, and cosurfactants were prepared and their pseudoternary-phase diagrams were constructed by water titration method. Seventeen dorzolamide hydrochloride nanoemulsions were prepared and evaluated for their physicochemical and drug release properties. These nanoemulsions showed acceptable physicochemical properties and exhibited slow drug release. Draize rabbit eye irritation test and histological examination were carried out for those preparations exhibiting superior properties and revealed that they were nonirritant. Biological evaluation of dorzolamide hydrochloride nanoemulsions on normotensive albino rabbits indicated that these products had higher therapeutic efficacy, faster onset of action, and prolonged effect relative to either drug solution or the market product. Formulation of dorzolamide hydrochloride in a nanoemulsion form offers, thus, a more intensive treatment of glaucoma, a decrease in the number of applications per day, and a better patient compliance compared to conventional eye drops.
authors.affiliation: Department of Pharmaceutical Technology, National Research Center, Dokki, Cairo, Egypt. husseinammar@hotmail.com
authors.forename: Hussein O
authors.initials: HO
authors.lastname: Ammar
authors.forename: H A
authors.initials: HA
authors.lastname: Salama
authors.forename: M
authors.initials: M
authors.lastname: Ghorab
authors.forename: A A
authors.initials: AA
authors.lastname: Mahmoud
mesh_terms: D000818:Animals; D001082:Aqueous Humor / Q000378:metabolism; D002257:Carbonic Anhydrase Inhibitors / Q000008:administration & dosage* / Q000009:adverse effects / Q000627:therapeutic use; D003315:Cornea / Q000378:metabolism; D016503:Drug Delivery Systems; D004355:Drug Stability; D004655:Emulsions; D005128:Eye Diseases / Q000139:chemically induced; D005901:Glaucoma / Q000188:drug therapy; D006863:Hydrogen-Ion Concentration; D007509:Irritants; D008297:Male; D053758:Nanoparticles; D009883:Ophthalmic Solutions; D009994:Osmolar Concentration; D010316:Particle Size; D011817:Rabbits; D012212:Rheology; D012995:Solubility; D013449:Sulfonamides / Q000008:administration & dosage* / Q000009:adverse effects / Q000627:therapeutic use; D013500:Surface Tension; D013876:Thiophenes / Q000008:administration & dosage* / Q000009:adverse effects / Q000627:therapeutic use; D014783:Viscosity
chemical_list: D002257:Carbonic Anhydrase Inhibitors; D004655:Emulsions; D007509:Irritants; D009883:Ophthalmic Solutions; D013449:Sulfonamides; D013876:Thiophenes; C062765:dorzolamide