April 2009
Volume 50, Issue 13
ARVO Annual Meeting Abstract  |   April 2009
Benzalkonium Chloride Homologs in Ocular Surface Cells in vitro and in vivo
Author Affiliations & Notes
  • P. O. Pellinen
    Preclinical Research, Santen Oy, Tampere, Finland
  • H. T. Uusitalo
    Department of Ophthalmology, University of Tampere, Tampere, Finland
    Department of Ophthalmology, Tampere University Hospital, Tampere, Finland
  • A. M. Huhtala
    Department of Ophthalmology, University of Tampere, Tampere, Finland
  • A. Tolonen
    Novamass Ltd, Oulu, Finland
  • Footnotes
    Commercial Relationships  P.O. Pellinen, Santen Oy, E; H.T. Uusitalo, Santen Oy, F; A.M. Huhtala, Santen Oy, F; A. Tolonen, Novamass Ltd, E.
  • Footnotes
    Support  Elsemay Björn Research Fund
Investigative Ophthalmology & Visual Science April 2009, Vol.50, 4070. doi:
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      P. O. Pellinen, H. T. Uusitalo, A. M. Huhtala, A. Tolonen; Benzalkonium Chloride Homologs in Ocular Surface Cells in vitro and in vivo. Invest. Ophthalmol. Vis. Sci. 2009;50(13):4070.

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      © ARVO (1962-2015); The Authors (2016-present)

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Purpose: : Ocular surface toxicity of commercial prostaglandin analogues seems to be related to the concentration of benzalkonium chloride (BAC) used as a preservative. BAC is a mixture of straight chain homologs and the proportions of these homologs in the mixture determine its effectiveness. The cytotoxic effects of different BAC homologs (BAC-C12, BAC-C14, BAC-C16) and BAC mixture (containing 64.1% C12, 33.8% C14, 2.1% C16) were studied in vitro in corneal and conjunctival epithelial cell cultures. In vivo in rabbit eyes, the distribution of BAC homologs in ocular surface tissues was examined.

Methods: : Human corneal epithelial (HCE) and human conjunctival epithelial (IOBA-NHC) cell cultures were exposed to BAC homologs or mixture for one hour. Cytotoxicity was assessed with the WST-1 assay for cellular growth and viability. BAC mixture as 0.02% (v/v) aqueous solution was applied into rabbit eyes once a day for 14 days and homologs in corneal and conjunctival tissues were analyzed using liquid chromatography-tandem mass spectrometry.

Results: : In vitro, conjunctival cells appeared to be more sensitive to BAC exposure than corneal cells. In corneal cells, the cytotoxicity for tested preservatives did not make much difference, with the EC50 values 0.00130% for C16, 0.00127% for BAC mixture, 0.00101% for C12, and 0.00097% for C14. In conjunctival cells, the EC50 values were 0.00065% for C16, 0.00047% for BAC mixture, 0.00041% for C14, and 0.00038% for C12. In vivo, the amounts of C12, C14 and C16 in corneal and conjunctival tissues were respectively (mean ± SEM, n=5): 0.37 ± 0.08 and 2.64 ± 0.27 ng/mg, 0.42 ± 0.07 and 4.77 ± 0.43 ng/mg, 0.04 ± 0.01 and 0.54 ± 0.05 ng/mg.

Conclusions: : Besides different potency of toxicity, BAC homologs possess different absorption kinetics in ocular surface tissues. The greater sensitivity of conjunctival cells than corneal cells in vitro may be explained by higher absorption of BAC homologs into the conjunctiva in vivo.

Keywords: ocular irritancy/toxicity testing • cornea: epithelium • conjunctiva 

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