title: Formulation strategy and evaluation of nanocrystal piroxicam orally disintegrating tablets manufacturing by freeze-drying.
abstract: Piroxicam (PRX) is a non-steroidal anti-inflammatory drug characterized by a poor water solubility and consequently by a low oral bioavailability. In this work, different nanocrystal orally disintegrating tablets (ODT) were prepared to enhance piroxicam dissolution rate and saturation solubility. PRX nanocrystals were prepared by means of high pressure homogenization technique using poloxamer 188 as stabilizer. Three different ODTs were prepared with the same nanosuspension using different excipients in order to study their effect on the PRX dissolution properties. PRX nanocrystal size and zeta potential were determined by photon correlation spectroscopy. Additional characterization of PRX nanocrystal ODT was carried out by infrared spectroscopy, X-ray powder diffractometry, differential scanning calorimetry. Dissolution study was performed in distilled water (pH 5.5) and compared with PRX coarse suspension ODT, PRX/poloxamer 188 physical mixture, bulk PRX samples and a PRX commercial ODT. All PRX nanocrystal ODT formulations showed a higher drug dissolution rate than coarse PRX ODT. PRX nanocrystal ODT prepared using gelatin or croscarmellose as excipient showed a higher PRX dissolution rate compared with the commercial formulation and ODT prepared using xanthan gum. Overall results confirmed that improved PRX dissolution rate is due to the increased surface-to-volume ratio due to the nanosized drug particle but also revealed the important role of different excipients used.
authors.affiliation: Dipartimento di Scienze della Vita e dell'Ambiente, Sezione di Scienze del Farmaco, CNBS, University of Cagliari, Cagliari 09124, Italy.
authors.forename: Francesco
authors.initials: F
authors.lastname: Lai
authors.affiliation: Dipartimento di Scienze Farmaceutiche-Sezione di Chimica Generale e Organica "A.Marchesini", University of Milan, Milan 20133, Italy.
authors.forename: Elena
authors.initials: E
authors.lastname: Pini
authors.affiliation: Dipartimento di Scienze della Vita e dell'Ambiente, Sezione di Scienze del Farmaco, CNBS, University of Cagliari, Cagliari 09124, Italy.
authors.forename: Francesco
authors.initials: F
authors.lastname: Corrias
authors.affiliation: Dipartimento di Scienze Farmaceutiche-Sezione di Chimica Generale e Organica "A.Marchesini", University of Milan, Milan 20133, Italy.
authors.forename: Jacopo
authors.initials: J
authors.lastname: Perricci
authors.affiliation: Dipartimento di Scienze della Vita e dell'Ambiente, Sezione di Scienze del Farmaco, CNBS, University of Cagliari, Cagliari 09124, Italy.
authors.forename: Maria
authors.initials: M
authors.lastname: Manconi
authors.affiliation: Dipartimento di Scienze della Vita e dell'Ambiente, Sezione di Scienze del Farmaco, CNBS, University of Cagliari, Cagliari 09124, Italy. Electronic address: mfadda@unica.it.
authors.forename: Anna Maria
authors.initials: AM
authors.lastname: Fadda
authors.affiliation: Dipartimento di Scienze della Vita e dell'Ambiente, Sezione di Scienze del Farmaco, CNBS, University of Cagliari, Cagliari 09124, Italy.
authors.forename: Chiara
authors.initials: C
authors.lastname: Sinico
mesh_terms: D000284:Administration, Oral; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage / Q000737:chemistry*; D002152:Calorimetry, Differential Scanning; D002266:Carboxymethylcellulose Sodium / Q000737:chemistry; D002626:Chemistry, Pharmaceutical; D018360:Crystallography, X-Ray; D005079:Excipients / Q000737:chemistry; D005612:Freeze Drying; D005780:Gelatin / Q000737:chemistry; D006863:Hydrogen-Ion Concentration; D007700:Kinetics; D053758:Nanoparticles; D036103:Nanotechnology; D010316:Particle Size; D010894:Piroxicam / Q000008:administration & dosage / Q000737:chemistry*; D020442:Poloxamer / Q000737:chemistry; D011135:Polysaccharides, Bacterial / Q000737:chemistry; D033362:Powder Diffraction; D012995:Solubility; D017550:Spectroscopy, Fourier Transform Infrared; D013607:Tablets; D013678:Technology, Pharmaceutical / Q000379:methods*
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D005079:Excipients; D011135:Polysaccharides, Bacterial; D013607:Tablets; D020442:Poloxamer; D010894:Piroxicam; D005780:Gelatin; D002266:Carboxymethylcellulose Sodium; C002563:xanthan gum
keywords: Aspartame (PubChem CID 134601); Croscarmellose (PubChem CID 24748); Excipients; Maltodextrin (PubChem CID 5793); Mannitol (PubChemCID 6251); Nanocrystal; Nanosuspensions; Orally disintegrating tablet; Piroxicam; Piroxicam (PubChem CID 54676228); Poloxamer 188 (PubChem CID 24751); Xanthan gum (PubChemCID 7107)