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 9 h, 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.
Lilia Catalanotti b, Marco Biondi d,e,⁎, Laura Mayol d,e
a Dipartimento di Scienze del Farmaco e Prodotti per la Salute, Università di Messina, Piazza Pugliatti 1, Messina, Italy
b Dipartimento di Ingegneria Chimica, dei Materiali e della Produzione Industriale, Università di Napoli Federico II, Piazzale V. Tecchio 80, 80125 Napoli, Italy
c Department of Abdominal Oncology, Istituto Nazionale per lo Studio e la Cura dei Tumori, Fondazione “G. Pascale”-IRCCS, Naples, Italy
d Dipartimento di Farmacia, Università di Napoli Federico II, Via D. Montesano 49, Napoli, Italy
e Interdisciplinary Research Centre on Biomaterials – CRIB – Università di Napoli Federico II, P.le Tecchio, 80, Napoli, Italy