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Molecules 2016, 21(5), 658; doi:10.3390/molecules21050658

Cytotoxicity of Different Excipients on RPMI 2650 Human Nasal Epithelial Cells

1
Department of Pharmaceutical Technology, University of Szeged, Eötvös u. 6, Szeged H-6720, Hungary
2
Goodwill Pharma Ltd., Cserzy Mihály u. 32, Szeged H-6724, Hungary
3
Institute of Biophysics, Biological Research Centre of the Hungarian Academy of Sciences, Temesvári körút 62, Szeged H-6726, Hungary
*
Author to whom correspondence should be addressed.
Academic Editors: Shufeng Zhou and Wei-Zhu Zhong
Received: 4 March 2016 / Revised: 6 May 2016 / Accepted: 16 May 2016 / Published: 18 May 2016
(This article belongs to the Special Issue Drug Design and Discovery: Principles and Applications)
View Full-Text   |   Download PDF [786 KB, uploaded 18 May 2016]   |  

Abstract

The nasal route receives a great deal of attention as a non-invasive method for the systemic administration of drugs. For nasal delivery, specific formulations containing excipients are used. Because of the sensitive respiratory mucosa, not only the active ingredients, but also additives need to be tested in appropriate models for toxicity. The aim of the study was to measure the cytotoxicity of six pharmaceutical excipients, which could help to reach larger residence time, better permeability, and increased solubility dissolution rate. The following excipients were investigated on RPMI 2650 human nasal septum tumor epithelial cells: β-d-mannitol, sodium hyaluronate, α and β-cyclodextrin, polyvinyl alcohol and methylcellulose. 3-(4,5-dimethyltiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) dye conversion assay and real-time impedance analysis were used to investigate cytotoxicity. No excipient showed toxicity at 0.3% (w/v) concentration or below while 1% concentration a significantly reduced metabolic activity was measured by MTT assay for methylcellulose and cyclodextrins. Using impedance measurements, only β-cyclodextrin (1%) was toxic to cells. Mannitol at 1% concentration had a barrier opening effect on epithelial cells, but caused no cellular damage. Based on the results, all additives at 0.3%, sodium hyaluronate and polyvinyl alcohol at 1% concentrations can be safely used for nasal formulations. View Full-Text
Keywords: nasal; cytotoxicity; nasal formulation; MTT dye assay; real-time impedance analysis nasal; cytotoxicity; nasal formulation; MTT dye assay; real-time impedance analysis
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

Horváth, T.; Bartos, C.; Bocsik, A.; Kiss, L.; Veszelka, S.; Deli, M.A.; Újhelyi, G.; Szabó-Révész, P.; Ambrus, R. Cytotoxicity of Different Excipients on RPMI 2650 Human Nasal Epithelial Cells. Molecules 2016, 21, 658.

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