title: In vitro and in vivo characterization of meloxicam nanoparticles designed for nasal administration.
abstract: The nasal pathway represents a non-invasive route for delivery of drugs to the systemic circulation. Nanonization of poorly soluble drugs offers a possibility to increase dissolution properties, epithelial permeability or even bioavailability. The aim of the present study was to use in vitro methods to screen formulations which were intended for nasal application, and to perform animal experiments for recognizing the differences in plasmakinetics of intranasal- and oral-administered meloxicam nanoparticles. Due to nanonization the solubility of meloxicam elevated up to 1.2mg/mL, additionally the extent of dissolution also increased, complete dissolution was observed in 15 min. Favorable in vitro diffusion profile of meloxicam nanoparticles was observed and their epithelial permeability through human RPMI2650 cells was elevated. The pharmacokinetic parameters were significantly increased when meloxicam was administered as nanoparticles to rats either nasally (increase of Cmax 2.7-fold, AUC 1.5-fold) or orally (increase of C(max) 2.4-fold, AUC 2-fold) as compared to physical mixture of the drug and the excipients.
authors.affiliation: Department of Pharmaceutical Technology, University of Szeged, Szeged, Hungary; Institute of Biophysics, Biological Research Centre of the Hungarian Academy of Sciences, Szeged, Hungary.
authors.forename: Levente
authors.initials: L
authors.lastname: Kürti
authors.forename: Róbert
authors.initials: R
authors.lastname: Gáspár
authors.forename: Árpád
authors.initials: Á
authors.lastname: Márki
authors.forename: Emese
authors.initials: E
authors.lastname: Kápolna
authors.forename: Alexandra
authors.initials: A
authors.lastname: Bocsik
authors.forename: Szilvia
authors.initials: S
authors.lastname: Veszelka
authors.forename: Csilla
authors.initials: C
authors.lastname: Bartos
authors.forename: Rita
authors.initials: R
authors.lastname: Ambrus
authors.forename: Monika
authors.initials: M
authors.lastname: Vastag
authors.forename: Mária A
authors.initials: MA
authors.lastname: Deli
authors.forename: Piroska
authors.initials: P
authors.lastname: Szabó-Révész
mesh_terms: D000281:Administration, Intranasal; D000284:Administration, Oral; D000818:Animals; D018929:Cell Culture Techniques; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects; D004337:Drug Carriers / Q000737:chemistry*; D006801:Humans; D008297:Male; D000077239:Meloxicam; D008567:Membranes, Artificial; D053758:Nanoparticles / Q000737:chemistry*; D009297:Nasal Mucosa / Q000166:cytology / Q000187:drug effects / Q000378:metabolism*; D010316:Particle Size; D010539:Permeability; D051381:Rats; D012995:Solubility; D013499:Surface Properties; D013816:Thermodynamics; D013843:Thiazines / Q000008:administration & dosage* / Q000097:blood / Q000493:pharmacokinetics / Q000633:toxicity; D013844:Thiazoles / Q000008:administration & dosage* / Q000097:blood / Q000493:pharmacokinetics / Q000633:toxicity
chemical_list: D004337:Drug Carriers; D008567:Membranes, Artificial; D013843:Thiazines; D013844:Thiazoles; D000077239:Meloxicam
keywords: Intranasal; Meloxicam; Nanoparticle; Nasal permeability; Pharmacokinetics; RPMI2650