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Drug absorption behavior after periocular injections.

H Sasaki1, S Kashiwagi, T Mukai

  • 1Department of Hospital Pharmacy, Nagasaki University School of Medicine, Japan.

Biological & Pharmaceutical Bulletin
|October 8, 1999
PubMed
Summary
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Periocular injections of ophthalmic drugs in rabbits show varied absorption based on route and volume. This method may effectively deliver drugs to eye tissues and the vitreous humor.

Area of Science:

  • Ophthalmology
  • Pharmacokinetics
  • Drug Delivery

Background:

  • Ophthalmic drug delivery to periocular tissues and the vitreous humor remains a challenge.
  • Understanding drug absorption after periocular injection is crucial for optimizing treatment strategies.

Purpose of the Study:

  • To investigate the absorption behavior of ophthalmic drugs following periocular injections in rabbits.
  • To compare the pharmacokinetic profiles of drugs administered via periocular injection versus topical instillation.

Main Methods:

  • Fluorescein isothiocyanate dextran (FITC-dextran) was used to study dye leakage into tear fluid after intracapsular, retrobulbar, and palpebral conjunctival injections.
  • High-performance liquid chromatography (HPLC) was employed to determine the concentrations of a model beta-blocker (Tisolol) in tear fluid, blood, aqueous humor, and vitreous body.

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Main Results:

  • Dye leakage into tears depended on injection route and volume.
  • Periocular injections resulted in faster systemic absorption and higher plasma AUC compared to instillation.
  • Tisolol showed lower AUC in the aqueous humor and higher vitreous humor to aqueous humor AUC ratio with periocular injection than with instillation.
  • Retrobulbar injection led to highest plasma and lowest ocular concentrations, while intracapsular injection showed the opposite.

Conclusions:

  • Periocular injections facilitate rapid systemic absorption due to rich vascularization.
  • This administration route may be effective for delivering drugs to periocular tissues and the vitreous body.
  • Injection route significantly influences drug distribution within ocular and systemic compartments.