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Related Experiment Videos

Pharmacokinetic differences between ocular inserts and eyedrops

S W Friedrich1, B A Saville, Y L Cheng

  • 1Department of1 Chemical Engineering and Applied Chemistry, University of Toronto, Canada.

Journal of Ocular Pharmacology and Therapeutics : the Official Journal of the Association for Ocular Pharmacology and Therapeutics
|January 1, 1996
PubMed
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Ocular inserts significantly increase drug absorption into the conjunctiva and iris-ciliary body compared to eye drops. This enhanced ocular drug delivery is due to reduced tear mixing and increased penetration across ocular tissues.

Area of Science:

  • Ophthalmology
  • Pharmacokinetics
  • Drug Delivery Systems

Background:

  • Controlled-release ocular inserts enhance drug absorption into the aqueous humor compared to eye drops.
  • Systemic drug absorption from ocular inserts depends on the drug's release rate.

Purpose of the Study:

  • To investigate the effect of ocular inserts on drug absorption into ocular tissues, specifically the conjunctiva and iris-ciliary body.
  • To compare ocular tissue drug absorption between ocular inserts and eye drop administration.

Main Methods:

  • Ocular absorption studies were conducted in albino rabbits using ethylene-vinyl acetate inserts containing timolol maleate.
  • A modified compartmental model, previously used for eye drop simulations, was employed to analyze ocular absorption.

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Main Results:

  • Conjunctival absorption was significantly higher with ocular inserts (2.7-fold increase in coefficient, 42-fold increase in AUC per mumol).
  • Iris-ciliary body absorption was 24 times higher with ocular inserts (AUC per mumol).
  • The iris-ciliary body AUC was 9 times greater than the aqueous humor AUC with inserts, versus 1.4 times with eye drops.

Conclusions:

  • Ocular inserts increase drug penetration into the conjunctiva and sclera, leading to greater absorption into the iris-ciliary body and aqueous humor.
  • Reduced tear mixing with ocular inserts contributes to higher local drug concentrations and subsequent tissue absorption.
  • Ocular inserts represent a more effective delivery method for increasing drug concentrations within ocular tissues compared to traditional eye drops.