title: Spontaneous arrangement of a tumor targeting hyaluronic acid shell on irinotecan loaded PLGA nanoparticles.
abstract: The arrangement of tumor targeting hyaluronic acid (HA) moieties on irinotecan (IRIN)-loaded poly(lactic-co-glycolic acid) (PLGA) nanoparticles (NPs) has been directed by means of a gradient of lipophilicity between the oil and water phases of the emulsion used to produce the NPs. PLGA constitutes the NP bulk while HA is superficially exposed, with amphiphilic poloxamers acting as a bridge between PLGA and HA. Differential scanning calorimetry, zeta potential analyses and ELISA tests were employed to support the hypothesis of polymer assembly in NP formulations. The presence of flexible HA chains on NP surface enhances NP size stability over time due to an increased electrostatic repulsion between NPs and a higher degree of hydration of the device surface. IRIN in vitro release kinetics can be sustained up to 7-13 days. In vitro biologic studies indicated that HA-containing NPs were more toxic than bare PLGA NPs against CD44-overexpressing breast carcinoma cells (HS578T), therefore indicating their ability to target CD44 receptor.
authors.affiliation: Dipartimento di Farmacia, Università di Napoli Federico II, Via D. Montesano 49, Napoli, Italy.
authors.forename: Simona
authors.initials: S
authors.lastname: Giarra
authors.affiliation: Dipartimento di Farmacia, Università di Napoli Federico II, Via D. Montesano 49, Napoli, Italy; Dipartimento di Scienze del Farmaco e dei Prodotti per la Salute, Università degli Studi di Messina, Viale Annunziata, 98100 Messina, Italy.
authors.forename: Carla
authors.initials: C
authors.lastname: Serri
authors.affiliation: Institute for Polymers, Composites and Biomaterials, National Research Council, Mostra d'Oltremare Pad. 20, Viale J. F. Kennedy 54, 80125 Napoli, Italy.
authors.forename: Luisa
authors.initials: L
authors.lastname: Russo
authors.affiliation: Institute for Polymers, Composites and Biomaterials, National Research Council, Mostra d'Oltremare Pad. 20, Viale J. F. Kennedy 54, 80125 Napoli, Italy.
authors.forename: Stefania
authors.initials: S
authors.lastname: Zeppetelli
authors.affiliation: Dipartimento di Farmacia, Università di Napoli Federico II, Via D. Montesano 49, Napoli, Italy; Interdisciplinary Research Centre on Biomaterials - CRIB, Università di Napoli Federico II, P.le Tecchio 80, Napoli, Italy.
authors.forename: Giuseppe
authors.initials: G
authors.lastname: De Rosa
authors.affiliation: Institute for Polymers, Composites and Biomaterials, National Research Council, Mostra d'Oltremare Pad. 20, Viale J. F. Kennedy 54, 80125 Napoli, Italy. Electronic address: bassunta@unina.it.
authors.forename: Assunta
authors.initials: A
authors.lastname: Borzacchiello
authors.affiliation: Dipartimento di Farmacia, Università di Napoli Federico II, Via D. Montesano 49, Napoli, Italy; Interdisciplinary Research Centre on Biomaterials - CRIB, Università di Napoli Federico II, P.le Tecchio 80, Napoli, Italy. Electronic address: mabiondi@unina.it.
authors.forename: Marco
authors.initials: M
authors.lastname: Biondi
authors.affiliation: Institute for Polymers, Composites and Biomaterials, National Research Council, Mostra d'Oltremare Pad. 20, Viale J. F. Kennedy 54, 80125 Napoli, Italy.
authors.forename: Luigi
authors.initials: L
authors.lastname: Ambrosio
authors.affiliation: Dipartimento di Farmacia, Università di Napoli Federico II, Via D. Montesano 49, Napoli, Italy; Interdisciplinary Research Centre on Biomaterials - CRIB, Università di Napoli Federico II, P.le Tecchio 80, Napoli, Italy.
authors.forename: Laura
authors.initials: L
authors.lastname: Mayol
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology; D002166:Camptothecin / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology; D045744:Cell Line, Tumor; D004337:Drug Carriers / Q000737:chemistry*; D065546:Drug Liberation; D006801:Humans; D018960:Hyaluronan Receptors / Q000378:metabolism; D006820:Hyaluronic Acid / Q000737:chemistry*; D000077146:Irinotecan; D019344:Lactic Acid / Q000737:chemistry*; D058990:Molecular Targeted Therapy; D053758:Nanoparticles / Q000737:chemistry*; D011100:Polyglycolic Acid / Q000737:chemistry*; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer
chemical_list: D000970:Antineoplastic Agents; D004337:Drug Carriers; D018960:Hyaluronan Receptors; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid; D000077146:Irinotecan; D006820:Hyaluronic Acid; D002166:Camptothecin
keywords: CD44; Hyaluronic acid; Nanoparticle; PLGA; Poloxamer; Tumor targeting