title: Surface modified zeolite-based granulates for the sustained release of diclofenac sodium.
abstract: In this study, a granulate for the oral controlled delivery of diclofenac sodium (DS), an anionic sparingly soluble nonsteroidal anti-inflammatory drug, has been realized by wet granulation, using a surface modified natural zeolite (SMNZ) as an excipient. The surface modification of the zeolite has been achieved by means of a cationic surfactant, so as to allow the loading of DS through ionic interaction and bestow a control over the drug release mechanism. The granules possessed a satisfactory dosage uniformity, a flowability suitable for an oral dosage form manufacturing, along with a sustained drug release up to 9h, driven by both ion exchange and transport kinetics. Furthermore, the obtained granulate did not elicit a significant cytotoxicity and could also induce a prolonged anti-inflammatory effect on RAW264.7 cells. Taking also into account that natural zeolites are generally abundant and economic, SMNZ can be considered as an attracting alternative excipient for the production of granules with sustained release features.
authors.affiliation: Dipartimento di Scienze del Farmaco e Prodotti per la Salute, Università di Messina, Piazza Pugliatti 1, Messina, Italy.
authors.forename: Carla
authors.initials: C
authors.lastname: Serri
authors.affiliation: Dipartimento di Ingegneria Chimica, dei Materiali e della Produzione Industriale, Università di Napoli Federico II, Piazzale V. Tecchio 80, 80125 Napoli, Italy.
authors.forename: Bruno
authors.initials: B
authors.lastname: de Gennaro
authors.affiliation: Department of Abdominal Oncology, Istituto Nazionale per lo Studio e la Cura dei Tumori, Fondazione "G. Pascale"-IRCCS, Naples, Italy.
authors.forename: Vincenzo
authors.initials: V
authors.lastname: Quagliariello
authors.affiliation: Department of Abdominal Oncology, Istituto Nazionale per lo Studio e la Cura dei Tumori, Fondazione "G. Pascale"-IRCCS, Naples, Italy.
authors.forename: Rosario Vincenzo
authors.initials: RV
authors.lastname: Iaffaioli
authors.affiliation: Dipartimento di Farmacia, Università di Napoli Federico II, Via D. Montesano 49, Napoli, Italy.
authors.forename: Giuseppe
authors.initials: G
authors.lastname: De Rosa
authors.affiliation: Dipartimento di Ingegneria Chimica, dei Materiali e della Produzione Industriale, Università di Napoli Federico II, Piazzale V. Tecchio 80, 80125 Napoli, Italy.
authors.forename: Lilia
authors.initials: L
authors.lastname: Catalanotti
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: 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: D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000737:chemistry; D002460:Cell Line; D003692:Delayed-Action Preparations / Q000737:chemistry*; D004008:Diclofenac / Q000737:chemistry*; D065546:Drug Liberation / Q000187:drug effects; D005079:Excipients / Q000737:chemistry; D007700:Kinetics; D051379:Mice; D013501:Surface-Active Agents / Q000737:chemistry; D017641:Zeolites / Q000737:chemistry*
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D003692:Delayed-Action Preparations; D005079:Excipients; D013501:Surface-Active Agents; D017641:Zeolites; D004008:Diclofenac
keywords: Cells; Diclofenac; Granulation; Sustained release; Zeolite