title: Niosomes containing hydroxyl additives as percutaneous penetration enhancers: effect on the transdermal delivery of sulfadiazine sodium salt.
abstract: The aim of this study was to improve the transdermal permeation of sulfadiazine sodium, employing synergistic combination of surfactants (in the form of niosomes) and additives with different number of hydroxylic groups, (following referred to as "alcohol"), as component of the bilayer. In particular the effect of different concentration of each alcohol (ethanol, propylene glycol or glycerol, from 5%, to 40% v/v) on niosomes size and distribution, drug entrapment efficiencies and ex vivo drug percutaneous permeation were evaluated, identifying formulations giving the best performances. The findings revealed that the presence of alcohol critically affect the physico-chemical properties of niosomes, with regards to dimensions, drug encapsulation and permeation. Vesicular size increased with the amount of alcohol and at the same alcohol concentration, follow the sequence ethanol>propylene glycol>glycerol. Loaded niosomes were larger than empty ones. Low E% values were found for ethanol, even less in propylene glycol and glycerol based samples, confirming that the chemical structure of the alcohol and its physico-chemical properties, affected the sulfadiazine entrapment efficiency. The comparative evaluation of percutaneous permeation profiles showed that the cumulative amount of permeated drug increases with alcohol concentration up to 20% v/v. Higher concentration (40% v/v) resulted in a strong decrease of the potential skin permeation. Best performances were obtained with glycerol. In all cases ex vivo sulfadiazine percutaneous permeations are controlled and improved respect to the corresponding free drug solutions and traditional niosomes used as controls.
authors.affiliation: Dipartimento di Farmacia e Scienze della Salute e della Nutrizione, Università della Calabria, Edificio Polifunzionale, 87036 Arcavacata di Rende, Cosenza, Italy. Electronic address: rita.muzzalupo@unical.it.
authors.forename: Rita
authors.initials: R
authors.lastname: Muzzalupo
authors.affiliation: Dipartimento di Farmacia e Scienze della Salute e della Nutrizione, Università della Calabria, Edificio Polifunzionale, 87036 Arcavacata di Rende, Cosenza, Italy; Dipartimento di Ingegneria Informatica, Modellistica, Elettronica e Sistemistica, Università della Calabria, Via P. Bucci Cubo 39/C, 87036 Arcavacata di Rende, Cosenza, Italy.
authors.forename: Lorena
authors.initials: L
authors.lastname: Tavano
authors.affiliation: Dipartimento Scienze della Vita e dell'Ambiente, Università degli Studi di Cagliari, Via Ospedale 72, 09124 Cagliari, Italy.
authors.forename: Francesco
authors.initials: F
authors.lastname: Lai
authors.affiliation: Dipartimento di Farmacia e Scienze della Salute e della Nutrizione, Università della Calabria, Edificio Polifunzionale, 87036 Arcavacata di Rende, Cosenza, Italy.
authors.forename: Nevio
authors.initials: N
authors.lastname: Picci
mesh_terms: D000431:Ethanol / Q000737:chemistry; D005990:Glycerol / Q000737:chemistry; D008081:Liposomes / Q000737:chemistry*; D046529:Microscopy, Electron, Transmission; D019946:Propylene Glycol / Q000737:chemistry; D013411:Sulfadiazine / Q000737:chemistry*; D013501:Surface-Active Agents / Q000737:chemistry*
chemical_list: D008081:Liposomes; D013501:Surface-Active Agents; D013411:Sulfadiazine; D000431:Ethanol; D019946:Propylene Glycol; D005990:Glycerol
keywords: Ethanol; Glycerol; Niosomes; Propylene glycol; Skin permeation; Sulfadiazine sodium