title: Solid lipid nanoparticles for the delivery of 1,3,5-triaza-7-phosphaadamantane (PTA) platinum (II) carboxylates.
abstract: The use of solid lipid nanoparticles (SLN) is a promising route for the delivery of platinum complexes aimed to anticancer activity. This paper describes the production and characterization of SLN suitable for the loading of Pt complexes containing the biocompatible phosphine 1,3,5-triaza-7-phosphaadamantane (PTA) as neutral ligand. After a screening of several lipidic phases, stearic acid-based SLN were identified as the most appropriate for the purpose. They were produced by emulsion-dilution method and then characterized in terms of dimension, polydispersity, time stability, pH balance and morphological aspect. Stearic acid SLN are designed as a system able to coordinate to platinum, acting as anionic carboxylic ligands, replacing the base carbonate of the Pt synthon [PtCO3(DMSO)2], where also DMSO can subsequently be substituted by phosphinic ligands, namely PTA. SLN functionalised with Pt-PTA were produced and characterized by this synthetic route. The toxicity of plain SLN and the antiproliferative effect of SLN functionalised with Pt-PTA were evaluated on two human cancer cell lines K562 and A2780. The results indicate that SLN can be exploited as a delivery system for Pt complexes with potential anticancer activity.
authors.affiliation: Department of Life Sciences & Biotechnology, University of Ferrara, Ferrara, Italy.
authors.forename: Maddalena
authors.initials: M
authors.lastname: Sguizzato
authors.affiliation: Department of Life Sciences & Biotechnology, University of Ferrara, Ferrara, Italy. Electronic address: crt@unife.it.
authors.forename: Rita
authors.initials: R
authors.lastname: Cortesi
authors.affiliation: Department of Life Sciences & Biotechnology, University of Ferrara, Ferrara, Italy.
authors.forename: Eleonora
authors.initials: E
authors.lastname: Gallerani
authors.affiliation: Macromolecular Chemistry II, University of Bayreuth, Germany.
authors.forename: Markus
authors.initials: M
authors.lastname: Drechsler
authors.affiliation: Department of Chemical and Pharmaceutical Sciences, University of Ferrara, Ferrara, Italy.
authors.forename: Lorenza
authors.initials: L
authors.lastname: Marvelli
authors.affiliation: Department of Life and Environmental Sciences, Università Politecnica delle Marche, Ancona, Italy.
authors.forename: Paolo
authors.initials: P
authors.lastname: Mariani
authors.affiliation: Department of Life and Environmental Sciences, Università Politecnica delle Marche, Ancona, Italy.
authors.forename: Federica
authors.initials: F
authors.lastname: Carducci
authors.affiliation: Department of Life Sciences & Biotechnology, University of Ferrara, Ferrara, Italy.
authors.forename: Riccardo
authors.initials: R
authors.lastname: Gavioli
authors.affiliation: Department of Life Sciences & Biotechnology, University of Ferrara, Ferrara, Italy.
authors.forename: Elisabetta
authors.initials: E
authors.lastname: Esposito
authors.affiliation: Department of Chemical and Pharmaceutical Sciences, University of Ferrara, Ferrara, Italy.
authors.forename: Paola
authors.initials: P
authors.lastname: Bergamini
mesh_terms: D000218:Adamantane / Q000031:analogs & derivatives / Q000737:chemistry; D000970:Antineoplastic Agents / Q000737:chemistry* / Q000633:toxicity; D002264:Carboxylic Acids / Q000737:chemistry; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D056831:Coordination Complexes / Q000737:chemistry* / Q000633:toxicity; D004337:Drug Carriers / Q000737:chemistry*; D004655:Emulsions / Q000737:chemistry; D006801:Humans; D020014:K562 Cells; D008055:Lipids / Q000737:chemistry*; D009682:Magnetic Resonance Spectroscopy; D053758:Nanoparticles / Q000737:chemistry*; D009943:Organophosphorus Compounds / Q000737:chemistry; D010316:Particle Size; D010984:Platinum / Q000737:chemistry; D013229:Stearic Acids / Q000737:chemistry
chemical_list: C501763:1,3,5-triaza-7-phosphaadamantane; D000970:Antineoplastic Agents; D002264:Carboxylic Acids; D056831:Coordination Complexes; D004337:Drug Carriers; D004655:Emulsions; D008055:Lipids; D009943:Organophosphorus Compounds; D013229:Stearic Acids; D010984:Platinum; C031183:stearic acid; D000218:Adamantane
keywords: Cancer; Delivery system; PTA; Platinum; Protonolysis; SLN