title: In vitro dissolution-permeation evaluation of an electrospun cyclodextrin-based formulation of aripiprazole using μFlux™.
abstract: Since it is a well-known fact that among the newly discovered active pharmaceutical ingredients the number of poorly water soluble candidates is continually increasing, dissolution enhancement of poorly water soluble drugs has become one of the central challenges of pharmaceutical studies. So far the preclinical studies have been mainly focused on formulation methods to enhance the dissolution of active compounds, in many cases disregarding the fact that the formulation matrix not only affects dissolution but also has an effect on the transport through biological membranes, changing permeation of the drug molecules. The aim of this study was to test an electrospun cyclodextrin-based formulation of aripiprazole with the novel μFlux apparatus, which monitors permeation together with dissolution, and by this means better in vitro-in vivo correlation is achieved. It was evinced that a cyclodextrin-based electrospun formulation of aripiprazole has the potential to ensure fast drug delivery through the oral mucosa owing to the ultrafast dissolution of the drug from the formulation and the enhanced flux across membranes as shown by the result of the novel in vitro dissolution and permeation test.
authors.affiliation: Budapest University of Technology and Economics, Department of Organic Chemistry and Technology, Hungary.
authors.forename: Enikő
authors.initials: E
authors.lastname: Borbás
authors.affiliation: Budapest University of Technology and Economics, Department of Organic Chemistry and Technology, Hungary.
authors.forename: Attila
authors.initials: A
authors.lastname: Balogh
authors.affiliation: Budapest University of Technology and Economics, Department of Organic Chemistry and Technology, Hungary.
authors.forename: Katalin
authors.initials: K
authors.lastname: Bocz
authors.affiliation: Budapest University of Technology and Economics, Department of Organic Chemistry and Technology, Hungary.
authors.forename: Judit
authors.initials: J
authors.lastname: Müller
authors.affiliation: Budapest University of Technology and Economics, Department of Organic Chemistry and Technology, Hungary.
authors.forename: Éva
authors.initials: É
authors.lastname: Kiserdei
authors.affiliation: Budapest University of Technology and Economics, Department of Organic Chemistry and Technology, Hungary.
authors.forename: Tamás
authors.initials: T
authors.lastname: Vigh
authors.affiliation: PION Inc., USA.
authors.forename: Bálint
authors.initials: B
authors.lastname: Sinkó
authors.affiliation: Semmelweis University, Department of Pharmaceutical Chemistry, Hungary.
authors.forename: Attila
authors.initials: A
authors.lastname: Marosi
authors.affiliation: Gedeon Richter Plc., Department of Discovery Pharmacokinetics, Hungary.
authors.forename: Attila
authors.initials: A
authors.lastname: Halász
authors.affiliation: Gedeon Richter Plc., Department of Discovery Pharmacokinetics, Hungary.
authors.forename: Zoltán
authors.initials: Z
authors.lastname: Dohányos
authors.affiliation: CYCLOLAB, Cyclodextrin Research and Development Laboratory Ltd., Hungary.
authors.forename: Lajos
authors.initials: L
authors.lastname: Szente
authors.affiliation: Gedeon Richter Plc., Compound Profiling Laboratory, Hungary. Electronic address: gy.balogh@richter.hu.
authors.forename: György T
authors.initials: GT
authors.lastname: Balogh
authors.affiliation: Budapest University of Technology and Economics, Department of Organic Chemistry and Technology, Hungary. Electronic address: zsknagy@oct.bme.hu.
authors.forename: Zsombor K
authors.initials: ZK
authors.lastname: Nagy
mesh_terms: D000328:Adult; D000465:Algorithms; D014150:Antipsychotic Agents / Q000008:administration & dosage* / Q000737:chemistry*; D000068180:Aripiprazole / Q000008:administration & dosage* / Q000737:chemistry*; D002626:Chemistry, Pharmaceutical; D003505:Cyclodextrins / Q000737:chemistry*; D016503:Drug Delivery Systems; D006801:Humans; D008297:Male; D008567:Membranes, Artificial; D009061:Mouth Mucosa / Q000378:metabolism; D057139:Nanofibers; D010539:Permeability; D012995:Solubility; D013816:Thermodynamics; D055815:Young Adult
chemical_list: D014150:Antipsychotic Agents; D003505:Cyclodextrins; D008567:Membranes, Artificial; D000068180:Aripiprazole
keywords: Aripiprazole; Cyclodextrin; Dissolution-permeation; Electrospinning; Microflux; Nanofiber; Permeation