Please use this identifier to cite or link to this item: http://hdl.handle.net/10316/92842
Title: Optimization of levofloxacin-loaded crosslinked chitosan microspheres for inhaled aerosol therapy
Authors: Gaspar, M. C. 
Sousa, João José Martins Simões 
Pais, Alberto António Caria Canelas 
Cardoso, O. M. 
Murtinho, Dina Maria Bairrada 
Serra, M.E.S.
Tewes, F.
Olivier, J.-C.
Keywords: Aerosol; Chitosan; Crosslinking agents; Cystic Fibrosis; Experimental design; Levofloxacin; Lung delivery; Microspheres
Issue Date: 2015
Publisher: Elsevier
Project: info:eu-repo/grantAgreement/FCT/SFRH/SFRH/BD/80307/2011/PT/PULMONARY TARGETING AND BIOPHARMACEUTICAL EVALUATIONS OF ANTI-INFECTIVE DRUGS ADMINISTERED AS INNOVATIVE MICROSPHERE AEROSOLS 
Serial title, monograph or event: European Journal of Pharmaceutics and Biopharmaceutics
Volume: 96
Abstract: The aim of this work was the development of innovative levofloxacin-loaded swellable microspheres (MS) for the dry aerosol therapy of pulmonary chronicPseudomonas aeruginosainfections in Cystic Fibrosis patients. In a first step, a factorial design was applied to optimize formulations of chitosan-based MS with glutaraldehyde as crosslinker. After optimization, other crosslinkers (genipin, glutaric acid and glyceraldehyde) were tested. Analyses of MS included aerodynamic and swelling properties, morphology, drug loading, thermal and chemical characteristics,in vitroantibacterial activity and drug release studies. The prepared MS presented a drug content ranging from 39.8% to 50.8% of levofloxacin in an amorphous or dispersed state, antibacterial activity and fast release profiles. The highest degree of swelling was obtained for MS crosslinked with glutaric acid and genipin. These formulations also presented satisfactory aerodynamic properties, making them a promising alternative, in dry-powder inhalers, to levofloxacin solution for inhalation.
URI: http://hdl.handle.net/10316/92842
ISSN: 09396411
DOI: 10.1016/j.ejpb.2015.07.010
Rights: openAccess
Appears in Collections:FFUC- Artigos em Revistas Internacionais

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