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Design and evaluation of an intravesical delivery system for superficial bladder cancer: preparation of gemcitabine HCl-loaded chitosan–thioglycolic acid nanoparticles and comparison of chitosan/poloxamer gels as carriers

Authors Ay Şenyiğit Z, Karavana SY, İlem-Özdemir D, Çalışkan C, Waldner C, Şen S, Bernkop-Schnürch A, Baloğlu E

Received 5 August 2015

Accepted for publication 12 September 2015

Published 14 October 2015 Volume 2015:10(1) Pages 6493—6507


Checked for plagiarism Yes

Review by Single anonymous peer review

Peer reviewer comments 2

Editor who approved publication: Prof. Dr. Thomas J. Webster

Zeynep Ay Şenyiğit,1 Sinem Yaprak Karavana,1 Derya İlem-Özdemir,2 Çağrı Çalışkan,2 Claudia Waldner,3 Sait Şen,4 Andreas Bernkop-Schnürch,5 Esra Baloğlu1

1Faculty of Pharmacy, Department of Pharmaceutical Technology, Ege University, Bornova, İzmir, Turkey; 2Faculty of Pharmacy, Department of Radiopharmacy, Ege University, Bornova, İzmir, Turkey; 3ThioMatrix, Forschungs-Beratungs GmbH, Innsbruck, Austria; 4Faculty of Medicine, Department of Pathology, Ege University, Bornova, İzmir, Turkey; 5Institute of Pharmacy, Department of Pharmaceutical Technology, University of Innsbruck, Innsbruck, Austria

Abstract: This study aimed to develop an intravesical delivery system of gemcitabine HCl for superficial bladder cancer in order to provide a controlled release profile, to prolong the residence time, and to avoid drug elimination via urination. For this aim, bioadhesive nanoparticles were prepared with thiolated chitosan (chitosan–thioglycolic acid conjugate) and were dispersed in bioadhesive chitosan gel or in an in situ gelling poloxamer formulation in order to improve intravesical residence time. In addition, nanoparticle-loaded gels were diluted with artificial urine to mimic in vivo conditions in the bladder and were characterized regarding changes in gel structure. The obtained results showed that chitosan-thioglycolic acid nanoparticles with a mean diameter of 174.5±3.762 nm and zeta potential of 32.100±0.575 mV were successfully developed via ionotropic gelation and that the encapsulation efficiency of gemcitabine HCl was nearly 20%. In vitro/ex vivo characterization studies demonstrated that both nanoparticles and nanoparticle-loaded chitosan and poloxamer gels might be alternative carriers for intravesical administration of gemcitabine HCl, prolonging its residence time in the bladder and hence improving treatment efficacy. However, when the gel formulations were diluted with artificial urine, poloxamer gels lost their in situ gelling properties at body temperature, which is in conflict with the aimed formulation property. Therefore, 2% chitosan gel formulation was found to be a more promising carrier system for intravesical administration of nanoparticles.

Keywords: chitosan–TGA, nanoparticle, gemcitabine HCl, intravesical administration, chitosan, poloxamer, superficial bladder cancer

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