August 1993
Volume 34, Issue 9
Free
Articles  |   August 1993
Ocular absorption of topically applied FK506 from liposomal and oil formulations in the rabbit eye.
Author Affiliations
  • U Pleyer
    Jules Stein Eye Institute, UCLA School of Medicine.
  • S Lutz
    Jules Stein Eye Institute, UCLA School of Medicine.
  • W J Jusko
    Jules Stein Eye Institute, UCLA School of Medicine.
  • K D Nguyen
    Jules Stein Eye Institute, UCLA School of Medicine.
  • M Narawane
    Jules Stein Eye Institute, UCLA School of Medicine.
  • D Rückert
    Jules Stein Eye Institute, UCLA School of Medicine.
  • B J Mondino
    Jules Stein Eye Institute, UCLA School of Medicine.
  • V H Lee
    Jules Stein Eye Institute, UCLA School of Medicine.
  • K Nguyen
    Jules Stein Eye Institute, UCLA School of Medicine.
Investigative Ophthalmology & Visual Science August 1993, Vol.34, 2737-2742. doi:
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    • Get Citation

      U Pleyer, S Lutz, W J Jusko, K D Nguyen, M Narawane, D Rückert, B J Mondino, V H Lee, K Nguyen; Ocular absorption of topically applied FK506 from liposomal and oil formulations in the rabbit eye.. Invest. Ophthalmol. Vis. Sci. 1993;34(9):2737-2742.

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      © ARVO (1962-2015); The Authors (2016-present)

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Abstract

PURPOSE: To investigate the use of topically applied FK506, a new immunosuppressive compound, systemic and ocular absorption was determined in serum and various ocular tissues. METHODS: Two drops of 20 microliters FK506 were applied using oil dissolved (OD-FK506) or liposome-bound (LIP-FK506) drug. FK506 concentrations were measured at intervals of 30, 60, and 120 minutes by immunoassay. RESULTS: After application of OD-FK506, the highest concentrations of FK506 were found in the cornea and the conjunctiva (200-1200 ng/g) with substantial drug also present in anterior and posterior sclera. Relatively low concentrations were measured in the aqueous and vitreous humors (0.2-1.0 ng/g) of these animals. Using the same treatment regimen, LIP-FK506 was effective in delivering significantly higher drug concentrations (P < 0.05) to all ocular tissues and particularly aqueous humor (5-28 ng/g) and vitreous humor (12-22 ng/g) at all time points. During the observation period drug concentrations produced by LIP-FK506 remained well above the therapeutic range. FK506 levels were not detectable in serum (< 0.2 ng/ml) with either drug formulation. CONCLUSION: These findings indicate that liposomes may be a promising formulation for topical use of FK506 in ocular immune-mediated diseases.

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