title: Albumin Nanoparticles for Brain Delivery: A Comparison of Chemical versus Thermal Methods and in vivo Behavior.
abstract: Human serum albumin nanoparticles (NPs) have gained considerable attention owing to their high loading capacity for various drugs and the fact that they are well tolerated. The aim of this work was to investigate two different methods to produce NPs without the use of organic solvents and to obtain useful drug-delivery systems to cross the blood-brain barrier. NPs were obtained by coacervation, using both chemical and thermal cross-linking processes. They were developed and optimized to target brain tissues after parenteral administration in healthy rats. Furthermore, their distribution, cellular uptake, and fate were investigated in vivo after intracerebral injection in healthy rats. The toxicity of the developed carriers was estimated by behavioral tests. All NPs were chemically and physically characterized by dynamic light scattering, transmission electron microscopy, and high-performance liquid chromatography coupled with diode array and fluorimetric detectors. Their distribution and fate in the brain were evaluated by fluorescence microscopy. NPs were observed to be located in different brain tissues depending on the mode of injection, and did not induce an inflammatory response. Behavioral tests demonstrated no locomotor, explorative, or cognitive function impairment induced by the NPs.
authors.affiliation: Department of Chemistry, Building of Pharmaceutical Sciences, University of Florence, Via Ugo Schiff 6, 50019, Sesto Fiorentino, FI, Italy. mc.bergonzi@unifi.it.
authors.forename: Maria C
authors.identifier: http://orcid.org/0000-0001-5144-1330
authors.initials: MC
authors.lastname: Bergonzi
authors.affiliation: Department of Chemistry, Building of Pharmaceutical Sciences, University of Florence, Via Ugo Schiff 6, 50019, Sesto Fiorentino, FI, Italy.
authors.forename: Clizia
authors.initials: C
authors.lastname: Guccione
authors.affiliation: Department of Neuroscience, Psychology, Drug Research and Child Health, Division of Pharmacology and Toxicology, University of Florence, 50139, Florence, FI, Italy.
authors.forename: Cristina
authors.initials: C
authors.lastname: Grossi
authors.affiliation: Department of Chemistry, Building of Pharmaceutical Sciences, University of Florence, Via Ugo Schiff 6, 50019, Sesto Fiorentino, FI, Italy.
authors.forename: Vieri
authors.initials: V
authors.lastname: Piazzini
authors.affiliation: Department of Chemistry, Building of Pharmaceutical Sciences, University of Florence, Via Ugo Schiff 6, 50019, Sesto Fiorentino, FI, Italy.
authors.forename: Andrea
authors.initials: A
authors.lastname: Torracchi
authors.affiliation: Department of Neuroscience, Psychology, Drug Research and Child Health, Division of Pharmacology and Toxicology, University of Florence, 50139, Florence, FI, Italy.
authors.forename: Ilaria
authors.initials: I
authors.lastname: Luccarini
authors.affiliation: Department of Neuroscience, Psychology, Drug Research and Child Health, Division of Pharmacology and Toxicology, University of Florence, 50139, Florence, FI, Italy.
authors.forename: Fiorella
authors.initials: F
authors.lastname: Casamenti
authors.affiliation: Department of Chemistry, Building of Pharmaceutical Sciences, University of Florence, Via Ugo Schiff 6, 50019, Sesto Fiorentino, FI, Italy.
authors.forename: Anna R
authors.initials: AR
authors.lastname: Bilia
mesh_terms: D000818:Animals; D001921:Brain / Q000378:metabolism*; D016503:Drug Delivery Systems; D005260:Female; D005976:Glutaral / Q000008:administration & dosage / Q000737:chemistry; D008297:Male; D051379:Mice; D008810:Mice, Inbred C57BL; D015394:Molecular Structure; D053758:Nanoparticles / Q000008:administration & dosage* / Q000737:chemistry*; D051381:Rats; D017208:Rats, Wistar; D012709:Serum Albumin / Q000008:administration & dosage* / Q000737:chemistry*; D013696:Temperature
chemical_list: D012709:Serum Albumin; D005976:Glutaral
keywords: cross-linking; drug delivery; green chemistry; in vivo studies; nanoparticles