en
Scientific article
English

Ocular tolerance of absorption enhancers in ophthalmic preparations

Published inAAPS PharmSci, vol. 4, no. 1, p. 6-10
Publication date2002
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.

Keywords
  • Ocular absorption
  • Permeation enhancers
  • Confocal microscopy
  • Toxicity
Citation (ISO format)
FURRER, Pascal et al. Ocular tolerance of absorption enhancers in ophthalmic preparations. In: AAPS PharmSci, 2002, vol. 4, n° 1, p. 6–10. doi: 10.1208/ps040102
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Article (Published version)
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ISSN of the journal1522-1059
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