An ion-paired moxifloxacin nanosuspension eye drop provides improved prevention and treatment of ocular infection

Aditya Josyula, Revaz Omiadze, Kunal Parikh, Pranjali Kanvinde, Matthew B. Appell, Pratikkumar Patel, Hiwa Saeed, Yogesh Sutar, Nicole Anders, Ping He, Peter J. McDonnell, Justin Hanes, Abhijit A. Date, Laura M. Ensign

Research output: Contribution to journalArticlepeer-review

Abstract

There are numerous barriers to achieving effective intraocular drug administration, including the mucus layer protecting the ocular surface. For this reason, antibiotic eye drops must be used multiple times per day to prevent and treat ocular infections. Frequent eye drop use is inconvenient for patients, and lack of adherence to prescribed dosing regimens limits treatment efficacy and contributes to antibiotic resistance. Here, we describe an ion-pairing approach used to create an insoluble moxifloxacin–pamoate (MOX–PAM) complex for formulation into mucus-penetrating nanosuspension eye drops (MOX–PAM NS). The MOX–PAM NS provided a significant increase in ocular drug absorption, as measured by the area under the curve in cornea tissue and aqueous humor, compared to Vigamox in healthy rats. Prophylactic and treatment efficacy were evaluated in a rat model of ocular Staphylococcus aureus infection. A single drop of MOX–PAM NS was more effective than Vigamox, and completely prevented infection. Once a day dosing with MOX–PAM NS was similar, if not more effective, than three times a day dosing with Vigamox for treating S. aureus infection. The MOX–PAM NS provided increased intraocular antibiotic absorption and improved prevention and treatment of ocular keratitis, and the formulation approach is highly translational and clinically relevant.

Original languageEnglish (US)
Article numbere10238
JournalBioengineering and Translational Medicine
Volume6
Issue number3
DOIs
StatePublished - Sep 2021

Keywords

  • antibiotic
  • conjunctivitis
  • eye drop
  • keratitis
  • mucoinert
  • mucus-penetrating particles

ASJC Scopus subject areas

  • Biotechnology
  • Biomedical Engineering
  • Pharmaceutical Science

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