European Journal of Clinical Pharmacology

, Volume 55, Issue 4, pp 317–323

Improved penetration of aminoglycosides and fluoroquinolones into the aqueous humour of patients by means of Acuvue contact lenses

  • E.-M. Hehl
  • R. Beck
  • K. Luthard
  • R. Guthoff
  • B. Drewelow
PHARMACOKINETICS AND DISPOSITION

DOI: 10.1007/s002280050635

Cite this article as:
Hehl, E., Beck, R., Luthard, K. et al. E J Clin Pharmacol (1999) 55: 317. doi:10.1007/s002280050635

Abstract

Objectives: In order to improve the penetration of topically applied drugs in ophthalmology, the suitability of hydrophilic contact lenses (Acuvue, Vistacon, power −1.0 D) as a drug delivery system for antibiotics was tested. A prospective study was undertaken to determine the transcorneal penetration of five topically applied aminoglycosides and fluoroquinolones into the aqueous humour of patients.

Methods: Two hundred and sixty-five patients undergoing cataract extraction received 0.3% gentamicin, kanamycin, tobramycin, ciprofloxacin or ofloxacin solution by two different modes of administration: either as eye drops (nine drops every 15 min, starting 2 h prior to surgery) or by means of a drug delivery system (Acuvue contact lenses soaked for 1 h in eye drop solution without preservatives, 1–5 h prior to surgery). At the beginning of cataract extraction, 50–100 μl aqueous fluid was aspirated from the anterior chamber and immediately stored at −80 °C. Antibiotic concentrations were measured using fluorescence polarisation immuno-assays (aminoglycosides) or high-performance liquid chromatography (fluoroquinolones).

Results: After soaking for 1 h in 0.3% eye drop solutions, Acuvue contact lenses released about 190–250 μg aminoglycoside and ofloxacin and 1000 μg ciprofloxacin. These amounts are considerably lower or in the same order of magnitude than obtained with application of eye drops (1350 μg).

From the aminoglycosides tested, only gentamicin and tobramycin, but not kanamycin, were able to penetrate into the aqueous humour of patients. After the wearing of antibiotic-soaked lenses, mean aqueous humour concentrations were higher than after the use of eye drops. This difference reached significance in tobramycin (1.09 (1.30) μg · ml−1 vs 0.49 (0.79) μg · ml−1), ciprofloxacin (1.23 (0.60) μg · ml−1 vs 0.38 (0.33) μg · ml−1) and ofloxacin (5.55 (2.53) μg · ml−1 vs 0.56 (0.37) μg · ml−1).

The percentage of patients with aqueous humour concentration above the MIC90 of Staphylococcus epidermidis, the most common cause of postoperative endophthalmitis, was 92% and 100% after wearing ciprofloxacin- or ofloxacin-soaked lenses, respectively.

Conclusion: Gentamicin and tobramycin penetrated into the aqueous humour of patients, whereas kanamycin was not able to overcome the corneal barrier. Acuvue contact lenses soaked in 0.3% eye drop solutions can release sufficient amounts of gentamicin, ciprofloxacin and ofloxacin to produce bacteriostatic concentrations in the humor aquosus. Acuvue contact lenses can be recommended as a drug delivery system for fluoroquinolones.

Key words Aqueous humour penetrationFluoroquinolonesAminoglycosides

Copyright information

© Springer-Verlag Berlin Heidelberg 1999

Authors and Affiliations

  • E.-M. Hehl
    • 1
  • R. Beck
    • 2
  • K. Luthard
    • 2
  • R. Guthoff
    • 2
  • B. Drewelow
    • 1
  1. 1.Institute of Experimental and Clinical Pharmacology and Toxicology, Department Clinical Pharmacology, University of Rostock, D-18055 Rostock Germany Tel.: +49-381-494-5777; Fax: +49-381-494-5749DE
  2. 2.Eye Clinic, University of Rostock, GermanyDE