title: [¹¹C]diclofenac sodium: synthesis and PET assessment of transdermal penetration.
abstract: The aim of this work was to study the feasibility of using Positron Emission Tomography (PET) imaging as a new tool to detect transdermal penetration of topical drugs in human subjects. The compound used in the study is sodium 2-[(2,6-dichlorophenyl)amino]phenyl]acetate, better known as diclofenac sodium. This molecule belongs to the family of non-steroidal anti-inflammatory drugs and is considered one of the first choices among non-steroidal anti-inflammatory drugs for the treatment of inflammatory diseases; it is widely used and commercially present in a large number of pharmaceutical forms and formulations. (11)C-labeled diclofenac has been synthesized and coformulated, as an internal indicator, with a proprietary preparation based on the use of a sprayer. The radiolabeled preparation was topically administered to healthy volunteers, and PET imaging was used to evaluate transdermal penetration. Results obtained have demonstrated the efficacy of PET and radiolabeled tracers for the evaluation of transdermal penetration of active pharmaceutical ingredients as topical formulations.
authors.affiliation: CNR Institute of Clinical Physiology, Via Moruzzi 1, 56124 Pisa, Italy.
authors.forename: Debora
authors.initials: D
authors.lastname: Petroni
authors.forename: Luca
authors.initials: L
authors.lastname: Menichetti
authors.forename: Oreste
authors.initials: O
authors.lastname: Sorace
authors.forename: Michela
authors.initials: M
authors.lastname: Poli
authors.forename: Massimo
authors.initials: M
authors.lastname: Vanasia
authors.forename: Piero A
authors.initials: PA
authors.lastname: Salvadori
mesh_terms: D000279:Administration, Cutaneous; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage / Q000138:chemical synthesis* / Q000378:metabolism*; D002250:Carbon Radioisotopes; D002851:Chromatography, High Pressure Liquid; D004008:Diclofenac / Q000008:administration & dosage / Q000138:chemical synthesis* / Q000378:metabolism*; D005240:Feasibility Studies; D006801:Humans; D049268:Positron-Emission Tomography
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D002250:Carbon Radioisotopes; D004008:Diclofenac