title: Synthesis and in vivo evaluation of the biodistribution of a 18F-labeled conjugate gold-nanoparticle-peptide with potential biomedical application.
abstract: Gold nanoparticles (AuNPs) have been extensively used in biological applications because of their biocompatibility, size, and ease of characterization, as well as an extensive knowledge of their surface chemistry. These features make AuNPs readily exploitable for biomedical applications, including drug delivery and novel diagnostic and therapeutic approaches. In a previous work, we studied ex vivo distribution of the conjugate C(AuNP)-LPFFD for its potential uses in the treatment of Alzheimer's disease. In this study, we covalently labeled the conjugate with [(18)F]-fluorobenzoate to study the in vivo distribution of the AuNP by positron emission tomography (PET). After intravenous administration in rat, the highest concentration of the radiolabeled conjugate was found in the bladder and urine with a lower proportion in the intestine, demonstrating progressive accumulation compatible with biliary excretion of the conjugate. The conjugate also accumulated in the liver and spleen. PET imaging allowed us to study the in vivo biodistribution of the AuNPs in a noninvasive and sensitive way using a reduced number of animals. Our results show that AuNPs can be covalently and radioactively labeled for PET biodistribution studies.
authors.affiliation: Departamento de Química Farmacológica y Toxicológica, Facultad de Ciencias Químicas y Farmacéuticas, Universidad de Chile, Sergio Livingstone 1007, Independencia, Santiago, Chile.
authors.forename: Simon
authors.initials: S
authors.lastname: Guerrero
authors.forename: José Raul
authors.initials: JR
authors.lastname: Herance
authors.forename: Santiago
authors.initials: S
authors.lastname: Rojas
authors.forename: Juan F
authors.initials: JF
authors.lastname: Mena
authors.forename: Juan Domingo
authors.initials: JD
authors.lastname: Gispert
authors.forename: Gerardo A
authors.initials: GA
authors.lastname: Acosta
authors.forename: Fernando
authors.initials: F
authors.lastname: Albericio
authors.forename: Marcelo J
authors.initials: MJ
authors.lastname: Kogan
mesh_terms: D000818:Animals; D002851:Chromatography, High Pressure Liquid; D004353:Drug Evaluation, Preclinical; D005462:Fluorine Radioisotopes / Q000493:pharmacokinetics*; D006046:Gold / Q000737:chemistry*; D008297:Male; D053768:Metal Nanoparticles; D046529:Microscopy, Electron, Transmission; D010455:Peptides / Q000737:chemistry / Q000493:pharmacokinetics*; D049268:Positron-Emission Tomography; D051381:Rats; D017207:Rats, Sprague-Dawley; D013056:Spectrophotometry, Ultraviolet; D020349:Surface Plasmon Resonance; D014018:Tissue Distribution
chemical_list: D005462:Fluorine Radioisotopes; D010455:Peptides; D006046:Gold