title: Physicochemical characterization of atorvastatin calcium/ezetimibe amorphous nano-solid dispersions prepared by electrospraying method.
abstract: In the present study, electrospraying was applied as a novel method for the fabrication of amorphous nano-solid dispersions (N-SDs) of atorvastatin calcium (ATV), ezetimibe (EZT), and ATV/EZT combination as poorly water-soluble drugs. N-SDs were prepared using polyvinylpyrrolidone K30 as an amorphous carrier in 1:1 and 1:5 drug to polymer ratios and the total solid (including drug and polymer) concentrations of 10 and 20% (w/v). The prepared formulations were further investigated for their morphological, physicochemical, and dissolution properties. Scanning electron microscopy studies indicated that the morphology and diameter of the electrosprayed samples (ESs) were influenced by the solution concentration and drug:polymer ratio, so that an increase in the solution concentration resulted in fiber formation while an increase in the polymer ratio led to enhancement of the particle diameter. Differential scanning calorimetry and X-ray powder diffraction studies together with in vitro dissolution test revealed that the ESs were present in an amorphous form with improved dissolution properties. Infrared spectroscopic studies showed hydrogen-bonding interaction between the drug and polymer in ESs. Since the electrospraying method benefits from the both amorphization and nanosizing effect, this novel approach seems to be an efficient method for the fabrication of N-SDs of poorly water-soluble drugs.
authors.affiliation: a Drug Applied Research Center, Faculty of Pharmacy , Tabriz University of Medical Sciences , Tabriz , Iran.|b Students Research Committee , Tabriz University of Medical Sciences , Tabriz , Iran.
authors.forename: Azin
authors.initials: A
authors.lastname: Jahangiri
authors.affiliation: a Drug Applied Research Center, Faculty of Pharmacy , Tabriz University of Medical Sciences , Tabriz , Iran.
authors.forename: Mohammad
authors.initials: M
authors.lastname: Barzegar-Jalali
authors.affiliation: c Biotechnology Research Center, Faculty of Pharmacy , Tabriz University of Medical Sciences , Tabriz , Iran.
authors.forename: Yousef
authors.initials: Y
authors.lastname: Javadzadeh
authors.affiliation: a Drug Applied Research Center, Faculty of Pharmacy , Tabriz University of Medical Sciences , Tabriz , Iran.
authors.forename: Hamed
authors.initials: H
authors.lastname: Hamishehkar
authors.affiliation: a Drug Applied Research Center, Faculty of Pharmacy , Tabriz University of Medical Sciences , Tabriz , Iran.
authors.forename: Khosro
authors.initials: K
authors.lastname: Adibkia
mesh_terms: D000069059:Atorvastatin / Q000737:chemistry / Q000493:pharmacokinetics; D000069438:Ezetimibe / Q000737:chemistry / Q000493:pharmacokinetics; D053758:Nanoparticles / Q000737:chemistry*; D011205:Povidone / Q000737:chemistry*
chemical_list: D000069059:Atorvastatin; D000069438:Ezetimibe; D011205:Povidone
keywords: Amorphous; atorvastatin; electrospraying; ezetimibe; nano-solid dispersions