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Ocular tolerance of absorption enhancers in ophthalmic preparations

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Abstract

The use of absorption promoters is a way to improve the bioavailability and therapeutic response of topically applied ophthalmic drugs. The ocular tolerance of 9 potential absorption promoters was investigated as well as the influence of the enhancers' concentration on the ocular tolerance. The substances tested were instillated repetitively (4 times per day, during 3 days, and once just before examination) as aqueous solutions onto rabbit corneas. Fluorescein dyeing enabled us to specifically mark corneal damage that was observed by confocal microscopy. The degree of corneal injury was assessed with an image-processing system that calculated the total fluorescent areas. Confocal microscopy results showed the relatively good tolerance of permeation enhancers like dimethyl sulfoxide (DMSO), decamethonium, edetate, glycocholate, and cholate in contrast to the poorly tolerated saponin and fusidate. Increasing the promoters' concentration led generally to an increase in corneal lesions.

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Authors and Affiliations

  1. School of Pharmacy, Institute of Medicinal Chemistry, University of Lausanne, CH-1015, Lausanne, Switzerland

    Pascal Furrer & Joachim Michael Mayer

  2. Centre de recherche, Merck, Sharp and Dohme-Chibret, F-63203, Riom, France

    Bernard Plazonnet

  3. School of Pharmacy, Department of Pharmaceutics and Biopharmaceutics, University of Geneva, CH-1211, Geneva 4, Switzerland

    Robert Gurny

Authors
  1. Pascal Furrer
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  2. Joachim Michael Mayer
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  3. Bernard Plazonnet
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  4. Robert Gurny
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Published: January 21, 2002

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Furrer, P., Mayer, J.M., Plazonnet, B. et al. Ocular tolerance of absorption enhancers in ophthalmic preparations. AAPS PharmSci 4, 2 (2002). https://doi.org/10.1208/ps040102

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  • DOI: https://doi.org/10.1208/ps040102

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