title: Swellable floating tablet based on spray-dried casein nanoparticles: Near-infrared spectral characterization and floating matrix evaluation.
abstract: In this study, spray-dried alfuzosin hydrochloride (ALF)-loaded casein (CAS) nanoparticles were successfully used for the preparation of a swellable floating matrix via direct compression. The developed NIR calibration model was able to assess ALF and CAS levels in five different batches of drug-loaded nanoparticles. The calibration and prediction plots exhibited good linearity with correlation coefficients of more than 0.9. The standard error of calibration and cross-validation was less than 5% of the measured values, confirming the accuracy of the model. A linear relationship was obtained correlating the actual drug entrapped and the predicted values obtained from the NIR partial least squares regression model. The un-crosslinked tablet demonstrated a substantial weight gain (317% after 2h) and completely disintegrated after 3-4h whereas both 10 and 40% w/w genipin-crosslinked tablets showed lower weight gain (114 and 42% after 2h, respectively). A rapid floating of the tablets within 5-15min (compared to 45min for the marketed tablet) was observed, with maintained floating for 24h. Marketed and prepared tablets succeeded to prolong ALF release for 24h. The development of drug-loaded CAS nanoparticles using spray-drying represents a new alternative for the preparation of swellable floating tablets for prolonged drug release.
authors.affiliation: Department of Industrial Pharmacy, Faculty of Pharmacy, Alexandria University, Alexandria, Egypt; Cancer Nanotechnology Research Laboratory (CNRL), Faculty of Pharmacy, Alexandria University, Alexandria, Egypt. Electronic address: dr_ahmedelzoghby@yahoo.com.
authors.forename: Ahmed O
authors.initials: AO
authors.lastname: Elzoghby
authors.affiliation: BÜCHI Labortechnik AG, Flawil, Switzerland.
authors.forename: Branko Z
authors.initials: BZ
authors.lastname: Vranic
authors.affiliation: Department of Industrial Pharmacy, Faculty of Pharmacy, Alexandria University, Alexandria, Egypt.
authors.forename: Wael M
authors.initials: WM
authors.lastname: Samy
authors.affiliation: Department of Industrial Pharmacy, Faculty of Pharmacy, Alexandria University, Alexandria, Egypt.
authors.forename: Nazik A
authors.initials: NA
authors.lastname: Elgindy
mesh_terms: D002138:Calibration; D002364:Caseins / Q000737:chemistry*; D002626:Chemistry, Pharmaceutical / Q000379:methods; D004339:Drug Compounding / Q000379:methods; D039823:Iridoids / Q000737:chemistry; D053758:Nanoparticles / Q000737:chemistry*; D019265:Spectroscopy, Near-Infrared / Q000379:methods; D013607:Tablets / Q000737:chemistry*
chemical_list: D002364:Caseins; D039823:Iridoids; D013607:Tablets; C007834:genipin
keywords: Casein nanoparticles; Genipin-crosslinking; NIR spectroscopy; Prolonged release; Spray-drying; Swellable floating tablet