Evaluation of a delivery system providing long-term release of cyclosporine

P. Andrew Pearson, Glenn J. Jaffe, Daniel F. Martin, Ghassan J. Cordahi, Hans Grossniklaus, Elmar T. Schmeisser, Paul Ashton

Research output: Contribution to journalArticlepeer-review

70 Scopus citations


Objectives: To examine the clearance of cyclosporine after intravitreal injection and to assess the kinetics and toxic effects of an intravitreal device that provides sustained delivery of cyclosporine. Methods: Rabbits were divided into two groups to evaluate (1) the elimination kinetics after 1-μg and 10-μg intravitreal injections of cyclosporine and (2) the levels produced after implantation of a device that contained cyclosporine over 6 months. The toxic effects of the intravitreal device over 6 months were assessed in rabbits and cynomolgus monkeys. Results: After the 10-μg injection, the half-life was longer (10.8 hours vs 4.2 hours) and the distribution volume was smaller (1.7 mL vs 3.2 mL) than after the 1-μg injection. This difference can be attributed to saturable partitioning of the drug. The device resulted in a vitreous concentration of approximately 500 ng/mL throughout the study period. In the rabbit it resulted in reversible lens opacification and decreased b-wave amplitude. This toxic effect was not detected in the monkey. Conclusions: The device produces sustained intravitreal levels of cyclosporine. Although it was associated with reversible toxic effects in the rabbit, it was well tolerated in primates. Sustained-release implants are a promising new treatment for chronic uveitis.

Original languageEnglish
Pages (from-to)311-317
Number of pages7
JournalArchives of Ophthalmology
Issue number3
StatePublished - Mar 1996

Bibliographical note

Funding Information:
This study was supported by the Heed Ophthalmic Fellowship, Cleveland, Ohio (Dr Pearson); the Adler Foun¬ dation,Scarsdale,NY(DrJoffe);ResearchtoPreventBlind¬ ness Ine, New York, NY; by grantsandEY09106 (DrJaffé) tute,Bethesda,Md.and 09973(DrAshton)fromtheNationalEyeInsti¬

ASJC Scopus subject areas

  • Ophthalmology


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