Transscleral permeability of fluorescent-labeled antibiotics

James C Kao1, Dayle H Geroski, Henry F Edelhauser

  • 1Department of Ophthalmology, Emory University School of Medicine, Atlanta, GA, USA.

Abstract

Insights

Human sclera shows higher permeability to penicillin G than vancomycin or polymyxin B. This suggests transscleral antibiotic delivery may be a viable option for treating posterior segment eye infections.

Area of Science:

  • Ophthalmology
  • Pharmacology
  • Biomedical Engineering

Background:

  • Posterior segment intraocular infections pose treatment challenges.
  • Effective drug delivery to the posterior eye segment is crucial for successful treatment.
  • Transscleral drug delivery offers a potential non-invasive approach.

Purpose of the Study:

  • To investigate the in vitro transscleral permeability of key antibiotics.
  • To assess the potential of antibiotics to penetrate the sclera for posterior segment infections.

Main Methods:

  • Human scleral tissue mounted in a perfusion chamber.
  • Fluorescent-labeled antibiotics (vancomycin, polymyxin B, penicillin G) applied to the episcleral surface.
  • Perfusate collected and analyzed for antibiotic diffusion using fluorometry.

Main Results:

  • Penicillin G exhibited significantly higher transscleral permeability (Ktrans: 1.89 x 10(-6) cm/s) compared to vancomycin and polymyxin B.
  • Over 24 hours, 50.8% of penicillin G diffused across the sclera, versus 20.6% for vancomycin and 12.6% for polymyxin B.
  • Lower molecular weight, water-soluble antibiotics demonstrated greater scleral penetration.

Conclusions:

  • Human sclera permeability varies significantly among different antibiotics.
  • Penicillin G, a lower molecular weight antibiotic, penetrates the sclera more readily.
  • Transscleral drug delivery is a promising strategy for treating posterior segment ocular infections.

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