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

Publication ,  Journal Article
Pearson, PA; Jaffe, GJ; Martin, DF; Cordahi, GJ; Grossniklaus, H; Schmeisser, ET; Ashton, P
Published in: Arch Ophthalmol
March 1996

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-microgram and 10-microgram 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-microgram 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-microgram 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.

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Published In

Arch Ophthalmol

DOI

ISSN

0003-9950

Publication Date

March 1996

Volume

114

Issue

3

Start / End Page

311 / 317

Location

United States

Related Subject Headings

  • Vitreous Body
  • Tissue Distribution
  • Retina
  • Rabbits
  • Ophthalmology & Optometry
  • Male
  • Macaca fascicularis
  • Lens, Crystalline
  • Injections
  • Immunosuppressive Agents
 

Citation

APA
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Pearson, P. A., Jaffe, G. J., Martin, D. F., Cordahi, G. J., Grossniklaus, H., Schmeisser, E. T., & Ashton, P. (1996). Evaluation of a delivery system providing long-term release of cyclosporine. Arch Ophthalmol, 114(3), 311–317. https://doi.org/10.1001/archopht.1996.01100130307014
Pearson, P. A., G. J. Jaffe, D. F. Martin, G. J. Cordahi, H. Grossniklaus, E. T. Schmeisser, and P. Ashton. “Evaluation of a delivery system providing long-term release of cyclosporine.Arch Ophthalmol 114, no. 3 (March 1996): 311–17. https://doi.org/10.1001/archopht.1996.01100130307014.
Pearson PA, Jaffe GJ, Martin DF, Cordahi GJ, Grossniklaus H, Schmeisser ET, et al. Evaluation of a delivery system providing long-term release of cyclosporine. Arch Ophthalmol. 1996 Mar;114(3):311–7.
Pearson, P. A., et al. “Evaluation of a delivery system providing long-term release of cyclosporine.Arch Ophthalmol, vol. 114, no. 3, Mar. 1996, pp. 311–17. Pubmed, doi:10.1001/archopht.1996.01100130307014.
Pearson PA, Jaffe GJ, Martin DF, Cordahi GJ, Grossniklaus H, Schmeisser ET, Ashton P. Evaluation of a delivery system providing long-term release of cyclosporine. Arch Ophthalmol. 1996 Mar;114(3):311–317.

Published In

Arch Ophthalmol

DOI

ISSN

0003-9950

Publication Date

March 1996

Volume

114

Issue

3

Start / End Page

311 / 317

Location

United States

Related Subject Headings

  • Vitreous Body
  • Tissue Distribution
  • Retina
  • Rabbits
  • Ophthalmology & Optometry
  • Male
  • Macaca fascicularis
  • Lens, Crystalline
  • Injections
  • Immunosuppressive Agents