Vitreous and aqueous penetration of orally and topically administered moxifloxacin

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Masamichi Fukuda1, Naoko Shibata, Hiromi Osada

  • 1Department of Ophthalmology, Kanazawa Medical University, Uchinada, Japan. fukuda@kanazawa-med.ac.jp

Ophthalmic Research
|February 18, 2011
PubMed
Abstract

Insights

Topical moxifloxacin (MFLX) achieved higher aqueous humor concentrations in rabbits compared to oral administration. However, oral MFLX resulted in significantly higher intravitreal concentrations, exceeding therapeutic levels for ocular infections.

Area of Science:

  • Pharmacology
  • Ophthalmology
  • Drug Delivery

Background:

  • Moxifloxacin (MFLX) is a fluoroquinolone antibiotic used to treat bacterial eye infections.
  • Understanding the pharmacokinetic profile of MFLX after different administration routes is crucial for optimizing treatment strategies.

Purpose of the Study:

  • To compare the pharmacokinetics of moxifloxacin hydrochloride in rabbits following topical ocular and oral administration.
  • To evaluate the drug concentrations in aqueous humor, vitreous humor, and serum after each administration route.

Main Methods:

  • Rabbits received topical ophthalmic solutions of MFLX (0.5%) or oral MFLX (16 mg/kg).
  • Aqueous, vitreous, and serum samples were collected at various time points post-administration.
  • High-performance liquid chromatography (HPLC) was used to quantify MFLX concentrations.

Main Results:

  • Topical MFLX yielded higher peak concentrations in the aqueous humor (10.2 μg/ml) compared to oral administration (0.9 μg/ml).
  • Oral MFLX resulted in significantly higher concentrations in the vitreous humor (0.7 μg/ml) compared to topical administration (0.10 μg/ml).
  • Oral MFLX achieved vitreous concentrations approximately 7-fold higher than topical MFLX.

Conclusions:

  • Topical administration leads to superior MFLX concentrations in the aqueous humor.
  • Oral administration provides higher intravitreal MFLX concentrations, which are crucial for treating posterior segment ocular infections.
  • Oral MFLX concentrations in the aqueous humor surpassed the minimum inhibitory concentration (MIC90) for common ocular pathogens.

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