Analysis of a sustained release intravitreal codrug device of 5-FU and Tri-hydroxy steroid

A. Pearson, M. Howard, S. Capoor, T. Cynkowski, G. Cynkowska, P. Crooks, P. Ashton

Research output: Contribution to journalArticlepeer-review


Purpose: We are evaluateing a codrug of 5-FU and Tri-hydroxy steroid (THS) for use as an inhibitor of angiogenesis. This study evaluated in vitro release and intravitreal toxicity in an animal model. Methods: In vitro release from 2mm pellets was measured in bovine vitreous over 30 days by HPLC. 1.5 mm pellets were implanted in the right eye of 15 NZW rabbits. A sham procedure was performed in the left control eye of each of these animals. Toxicity was evaluated by serial clinical examinations and electroretinograms and animals were sacrificed for histopathological analysis at 9 weeks. Results: Apparent release of THS in bovine vitreous was 1 μg/day, Bis was released at 3.5μg/day and 5-FU release was 25μg/day. On clinical examination there was no evidence of toxicity. ERG's remained normal for the duration of the study. Visible codrug pellets were present at 9 weeks after implantation. Light microscopic analysis showed no evidence of retinal toxicity. Conclusions: This device provides sustained release in the vitreous for 30 days. This sustained release intravitreal codrug device is non-toxic to the rabbit eye. This route may be promising in the treatment of intraocular angiogenesis.

Original languageEnglish
Pages (from-to)S582
JournalInvestigative Ophthalmology and Visual Science
Issue number3
StatePublished - Feb 15 1996

ASJC Scopus subject areas

  • Ophthalmology
  • Sensory Systems
  • Cellular and Molecular Neuroscience


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