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Title: Effects of drug solubility, state and loading on controlled release in bicomponent electrospun fibers
Authors: Natu, Mădălina V. 
Sousa, Hermínio C. de 
Gil, M. H. 
Keywords: Electrospinning; Bicomponent fibers; Drug release; Modeling
Issue Date: Sep-2010
Publisher: Elsevier
Citation: NATU, Mădălina V.; SOUSA, Hermínio C. de; GIL, M. H. - Effects of drug solubility, state and loading on controlled release in bicomponent electrospun fibers. "International Journal of Pharmaceutics". ISSN 0378-5173. 397:1–2 (2010) 50–58
Serial title, monograph or event: International Journal of Pharmaceutics
Volume: 397
Issue: 1-2
Abstract: Bicomponent fibers of two semi-crystalline (co)polymers, poly(ɛ-caprolactone), and poly(oxyethylene-b-oxypropylene-b-oxyethylene), were obtained by electrospinning. Acetazolamide and timolol maleate were loaded in the fibers in different concentrations (below and above the drug solubility limit in polymer) in order to determine the effect of drug solubility in polymer, drug state, drug loading and fiber composition on fiber morphology, drug distribution and release kinetics. The high loadings fibers (with drug in crystalline form) showed higher burst and faster release than low drug content fibers, indicating the release was more sustained when the drug was encapsulated inside the fibers, in amorphous form. Moreover, timolol maleate was released faster than acetazolamide, indicating that drug solubility in polymer influences the partition of drug between polymer and elution medium, while fiber composition also controlled drug release. At low loadings, total release was not achieved (cumulative release percentages smaller than 100%), suggesting that drug remained trapped in the fibers. The modeling of release data implied a three stage release mechanism: a dissolution stage, a desorption and subsequent diffusion through water-filled pores, followed by polymer degradation control.
ISSN: 0378-5173
DOI: 10.1016/j.ijpharm.2010.06.045
Rights: openAccess
Appears in Collections:FCTUC Eng.Química - Artigos em Revistas Internacionais

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