title: Preparation and in vitro evaluation of chitosan nanoparticles containing a caspase inhibitor.
abstract: The aim of this work was to develop a formulation for Z-DEVD-FMK, a peptide which is a caspase inhibitor and has been used in experimental animal studies for a decade. Peptide loaded chitosan nanoparticles were obtained by ionotropic gelation process and Z-DEVD-FMK was quantified by an HPLC method. The influence of the initial peptide concentration on the nanoparticle characteristics and release behavior was evaluated. The CS nanoparticles have a particle diameter (Z-average) ranging from approximately 313-412 nm and a positive zeta potential (20-28 mV). The formulation with the initial peptide concentration of 400 ng/ml provided the highest loading capacity (0.46%) and the highest extent of release (65% at 24 h) suggesting the possibility to achieve a therapeutic dose. According to the data obtained, this chitosan-based nanotechnology opens new and interesting perspectives for anticaspase activity.
authors.affiliation: Department of Pharmaceutical Technology, Faculty of Pharmacy, Hacettepe University, 06100 Ankara, Turkey.
authors.forename: Yeşim
authors.initials: Y
authors.lastname: Aktaş
authors.forename: Karine
authors.initials: K
authors.lastname: Andrieux
authors.forename: Maria Jose
authors.initials: MJ
authors.lastname: Alonso
authors.forename: Pilar
authors.initials: P
authors.lastname: Calvo
authors.forename: R Neslihan
authors.initials: RN
authors.lastname: Gürsoy
authors.forename: Patrick
authors.initials: P
authors.lastname: Couvreur
authors.forename: Yilmaz
authors.initials: Y
authors.lastname: Capan
mesh_terms: D061945:Caspase Inhibitors; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D048271:Chitosan / Q000737:chemistry*; D002851:Chromatography, High Pressure Liquid; D004563:Electrochemistry; D005782:Gels; D046529:Microscopy, Electron, Transmission; D049329:Nanostructures; D009842:Oligopeptides / Q000008:administration & dosage* / Q000737:chemistry; D010316:Particle Size; D011480:Protease Inhibitors / Q000008:administration & dosage* / Q000737:chemistry
chemical_list: D061945:Caspase Inhibitors; D005782:Gels; D009842:Oligopeptides; D011480:Protease Inhibitors; C110772:benzoylcarbonyl-aspartyl-glutamyl-valyl-aspartyl-fluoromethyl ketone; D048271:Chitosan