Oxygen-Carrying Capacity of Perfluorohexyloctane, a Novel Eye Drop for Dry Eye Disease

ABSTRACT: Objective: One-hundred percent perfluorohexyloctane (PFHO) is a water-free, preservative-free eye drop approved by the Food and Drug Administration in the United States for the treatment of dry eye disease. PFHO has shown relief of dry eye signs and symptoms in clinical trials and has pot...

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Main Authors: Neal Stolowich, Ph.D., Jason Vittitow, Ph.D., Robert Kissling, M.D., Douglas Borchman, Ph.D.
Format: Article
Language:English
Published: Elsevier 2023-01-01
Series:Current Therapeutic Research
Subjects:
Online Access:http://www.sciencedirect.com/science/article/pii/S0011393X23000140
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author Neal Stolowich, Ph.D.
Jason Vittitow, Ph.D.
Robert Kissling, M.D.
Douglas Borchman, Ph.D.
author_facet Neal Stolowich, Ph.D.
Jason Vittitow, Ph.D.
Robert Kissling, M.D.
Douglas Borchman, Ph.D.
author_sort Neal Stolowich, Ph.D.
collection DOAJ
description ABSTRACT: Objective: One-hundred percent perfluorohexyloctane (PFHO) is a water-free, preservative-free eye drop approved by the Food and Drug Administration in the United States for the treatment of dry eye disease. PFHO has shown relief of dry eye signs and symptoms in clinical trials and has potent antievaporative action in vitro. The objective of this study was to measure the level of oxygen in PFHO. Methods: T1 relaxation times (time taken for proton spins to translate from a random alignment to an alignment with the main magnetic field) for fluorine-19 in perfluorohexyloctane were measured using fluorine-19 nuclear magnetic resonance spectroscopy. The level of oxygen was interpolated from published data. Results: The hydrogen-1 and fluorine-19 nuclear magnetic resonance spectra of PFHO were well resolved and the resonance assignments and intensities were as expected. The T1 values calculated for the CF3 group resonance in the current study was 0.901 seconds and 1.12 seconds at 25 °C and 37 °C, respectively. The T1 values for the CF2 group resonances increased by 17% to 24% with an increase in temperature from 25 °C to 37 °C. The mean (SD) partial pressure of oxygen in PFHO was calculated to be 257 (36) mm Hg and 270 (38) mm Hg at 25 °C and 37 °C, respectively. Conclusions: The current study confirms that PFHO contains a significant amount of oxygen, more so than that calculated for tears in equilibrium with air. Once instilled on the eye, PFHO is not expected to be a barrier to the oxygen necessary for a healthy cornea and may in fact deliver nonreactive oxygen to the cornea to facilitate healing in patients with dry eye disease.
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spelling doaj.art-ded10b4e5a2a43649db782e8f3ee55b22023-06-21T06:50:46ZengElsevierCurrent Therapeutic Research0011-393X2023-01-0198100705Oxygen-Carrying Capacity of Perfluorohexyloctane, a Novel Eye Drop for Dry Eye DiseaseNeal Stolowich, Ph.D.0Jason Vittitow, Ph.D.1Robert Kissling, M.D.2Douglas Borchman, Ph.D.3Department of Chemistry, University of Louisville, Louisville, KentuckyClinical Affairs, Bausch + Lomb, Bridgewater, New JerseyMedical Affairs, Bausch + Lomb, Bridgewater, New JerseyDepartment of Ophthalmology and Visual Sciences, University of Louisville, Louisville, Kentucky; Address correspondence to: Douglas Borchman, Ph.D., Department of Ophthalmology and Visual Sciences, The University of Louisville, 301 E Muhammad Ali Blvd, Louisville, KY 40202.ABSTRACT: Objective: One-hundred percent perfluorohexyloctane (PFHO) is a water-free, preservative-free eye drop approved by the Food and Drug Administration in the United States for the treatment of dry eye disease. PFHO has shown relief of dry eye signs and symptoms in clinical trials and has potent antievaporative action in vitro. The objective of this study was to measure the level of oxygen in PFHO. Methods: T1 relaxation times (time taken for proton spins to translate from a random alignment to an alignment with the main magnetic field) for fluorine-19 in perfluorohexyloctane were measured using fluorine-19 nuclear magnetic resonance spectroscopy. The level of oxygen was interpolated from published data. Results: The hydrogen-1 and fluorine-19 nuclear magnetic resonance spectra of PFHO were well resolved and the resonance assignments and intensities were as expected. The T1 values calculated for the CF3 group resonance in the current study was 0.901 seconds and 1.12 seconds at 25 °C and 37 °C, respectively. The T1 values for the CF2 group resonances increased by 17% to 24% with an increase in temperature from 25 °C to 37 °C. The mean (SD) partial pressure of oxygen in PFHO was calculated to be 257 (36) mm Hg and 270 (38) mm Hg at 25 °C and 37 °C, respectively. Conclusions: The current study confirms that PFHO contains a significant amount of oxygen, more so than that calculated for tears in equilibrium with air. Once instilled on the eye, PFHO is not expected to be a barrier to the oxygen necessary for a healthy cornea and may in fact deliver nonreactive oxygen to the cornea to facilitate healing in patients with dry eye disease.http://www.sciencedirect.com/science/article/pii/S0011393X23000140CorneaDry eyeEye dropNMROxygenPerfluorhexyloctane
spellingShingle Neal Stolowich, Ph.D.
Jason Vittitow, Ph.D.
Robert Kissling, M.D.
Douglas Borchman, Ph.D.
Oxygen-Carrying Capacity of Perfluorohexyloctane, a Novel Eye Drop for Dry Eye Disease
Current Therapeutic Research
Cornea
Dry eye
Eye drop
NMR
Oxygen
Perfluorhexyloctane
title Oxygen-Carrying Capacity of Perfluorohexyloctane, a Novel Eye Drop for Dry Eye Disease
title_full Oxygen-Carrying Capacity of Perfluorohexyloctane, a Novel Eye Drop for Dry Eye Disease
title_fullStr Oxygen-Carrying Capacity of Perfluorohexyloctane, a Novel Eye Drop for Dry Eye Disease
title_full_unstemmed Oxygen-Carrying Capacity of Perfluorohexyloctane, a Novel Eye Drop for Dry Eye Disease
title_short Oxygen-Carrying Capacity of Perfluorohexyloctane, a Novel Eye Drop for Dry Eye Disease
title_sort oxygen carrying capacity of perfluorohexyloctane a novel eye drop for dry eye disease
topic Cornea
Dry eye
Eye drop
NMR
Oxygen
Perfluorhexyloctane
url http://www.sciencedirect.com/science/article/pii/S0011393X23000140
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