title: Preparation, characterization and in vitro activities evaluation of solid lipid nanoparticles based on PEG-40 stearate for antifungal drugs vaginal delivery.
abstract: The present article reports the preparation, characterization and performance evaluation of solid lipid nanoparticles (SLNs) based on polyoxyethylene-40 stearate (PEG-40 stearate) for the administration of antifungal agents such as ketoconazole and clotrimazole. These nanoparticles could be useful in the treatment of vaginal infections sustained by Candida albicans. In particular, PEG-40 stearate was made to react with acryloyl chloride in order to introduce an easily polymerizable moiety for the creation of a second shell and to ensure a slow drug release. In addition, the differences on the release profiles between PEG-40 stearate-based nanoparticles, PEG-40 stearate acrylate based and polymerized ones, were analyzed under conditions, simulating the typical environment of Candida albicans infection. Then, the antifungal activity of nanoparticles was also evaluated in terms of minimal inhibitory concentration. Moreover, the nanoparticles were submitted to in vitro studies for evaluating the drug permeability at the site of action. Results indicated that the obtained particles are potentially useful for the treatment of vaginal infections sustained by Candida albicans.
authors.affiliation: a Department of Pharmaceutical Sciences , University of Calabria , Arcavacata di Rende , Cosenza , Italy and.
authors.forename: Roberta
authors.initials: R
authors.lastname: Cassano
authors.affiliation: a Department of Pharmaceutical Sciences , University of Calabria , Arcavacata di Rende , Cosenza , Italy and.
authors.forename: Teresa
authors.initials: T
authors.lastname: Ferrarelli
authors.affiliation: b Virology and Microbiology Service of "Annunziata" Hospital , Cosenza , Italy.
authors.forename: Maria Vittoria
authors.initials: MV
authors.lastname: Mauro
authors.affiliation: b Virology and Microbiology Service of "Annunziata" Hospital , Cosenza , Italy.
authors.forename: Paolina
authors.initials: P
authors.lastname: Cavalcanti
authors.affiliation: a Department of Pharmaceutical Sciences , University of Calabria , Arcavacata di Rende , Cosenza , Italy and.
authors.forename: Nevio
authors.initials: N
authors.lastname: Picci
authors.affiliation: a Department of Pharmaceutical Sciences , University of Calabria , Arcavacata di Rende , Cosenza , Italy and.
authors.forename: Sonia
authors.initials: S
authors.lastname: Trombino
mesh_terms: D000179:Acrylates / Q000737:chemistry; D000935:Antifungal Agents / Q000737:chemistry* / Q000494:pharmacology; D002176:Candida albicans / Q000187:drug effects; D002460:Cell Line; D003022:Clotrimazole / Q000737:chemistry / Q000494:pharmacology; D003692:Delayed-Action Preparations / Q000737:chemistry / Q000494:pharmacology; D004337:Drug Carriers / Q000737:chemistry; D016503:Drug Delivery Systems / Q000379:methods; D005260:Female; D006801:Humans; D007654:Ketoconazole / Q000737:chemistry / Q000494:pharmacology; D008055:Lipids / Q000737:chemistry*; D008826:Microbial Sensitivity Tests / Q000379:methods; D053758:Nanoparticles / Q000737:chemistry*; D011092:Polyethylene Glycols / Q000737:chemistry*; D014621:Vagina / Q000378:metabolism*
chemical_list: D000179:Acrylates; D000935:Antifungal Agents; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D008055:Lipids; C526284:polyoxyethylene 40 stearate; D011092:Polyethylene Glycols; C026200:acryloyl chloride; D003022:Clotrimazole; D007654:Ketoconazole
keywords: Antifungal activity; polymerization; polyoxyethylene-40 stearate; solid lipid nanoparticles; vaginal release