title: Preparation and characterization of nanofibrous sheets for enhanced oral dissolution of nebivolol hydrochloride.
abstract: Nebivolol-loaded electrospun nanofibrous sheets were prepared for the dissolution enhancement of the active with the aim of improving its oral bioavailability. Physicochemical characterization of nanofibers including differential scanning calorimetry, attenuated total reflectance Fourier transform infrared spectroscopy and positron annihilation lifetime spectroscopy were carried out in order to track the physicochemical changes related to the electrospinning process. The obtained results unanimously indicated the amorphous transition of nebivolol as a result of electrospinning, furthermore supramolecular ordering of chains of polyvinyl alcohol matrix could be revealed by positron annihilation lifetime spectroscopy. The crystalline-amorphous conversion of the active, along with the increased specific surface area of the nanofibers enabled rapid and complete dissolution. More than twice amount of active released from the fibrous sheets than from the commercial tablets. In contrast to the control tablets, the dissolution was complete and was not influenced by the pH of the applied media.
authors.affiliation: Department of Pharmaceutical Industry and Management, University of Medicine and Pharmacy of Tîrgu Mureș, R-540139, Marinescu Street 38, Tirgu Mureș, Romania.
authors.forename: Emese
authors.initials: E
authors.lastname: Sipos
authors.affiliation: Department of Pharmaceutical Industry and Management, University of Medicine and Pharmacy of Tîrgu Mureș, R-540139, Marinescu Street 38, Tirgu Mureș, Romania.
authors.forename: Zoltán István
authors.initials: ZI
authors.lastname: Szabó
authors.affiliation: Department of Pharmaceutical Technology, University of Medicine and Pharmacy of Tîrgu Mureș, R-540139, Marinescu Street 38, Tirgu Mureș, Romania.
authors.forename: Emőke
authors.initials: E
authors.lastname: Rédai
authors.affiliation: University Pharmacy Department of Pharmacy Administration, Semmelweis University, Hőgyes Endre Str. 7-9, H-1092, Budapest, Hungary; Gedeon Richter Plc., Formulation R&D, Gyömrői Str. 19-21, H-1103 Budapest, Hungary.
authors.forename: Péter
authors.initials: P
authors.lastname: Szabó
authors.affiliation: University Pharmacy Department of Pharmacy Administration, Semmelweis University, Hőgyes Endre Str. 7-9, H-1092, Budapest, Hungary.
authors.forename: István
authors.initials: I
authors.lastname: Sebe
authors.affiliation: University Pharmacy Department of Pharmacy Administration, Semmelweis University, Hőgyes Endre Str. 7-9, H-1092, Budapest, Hungary. Electronic address: zelko.romana@pharma.semmelweis-univ.hu.
authors.forename: Romána
authors.initials: R
authors.lastname: Zelkó
mesh_terms: D000284:Administration, Oral; D001682:Biological Availability; D002152:Calorimetry, Differential Scanning / Q000379:methods; D006863:Hydrogen-Ion Concentration; D057139:Nanofibers / Q000737:chemistry*; D000068577:Nebivolol / Q000737:chemistry*; D011142:Polyvinyl Alcohol / Q000737:chemistry; D012995:Solubility; D017550:Spectroscopy, Fourier Transform Infrared / Q000379:methods; D013607:Tablets / Q000737:chemistry
chemical_list: D013607:Tablets; D000068577:Nebivolol; D011142:Polyvinyl Alcohol
keywords: Differential scanning calorimetry (DSC); Dissolution enhancement; Electrospinning; Nanofibers; Nebivolol hydrochloride; Positron annihilation lifetime spectroscopy (PALS)