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An Ilomastat-CD Eye Drop Formulation to Treat Ocular Scarring

Mohamed-Ahmed, AHA; Lockwood, A; Li, H; Bailly, M; Khaw, PT; Brocchini, S; (2017) An Ilomastat-CD Eye Drop Formulation to Treat Ocular Scarring. Investigative Ophthalmology & Visual Science , 58 (9) pp. 3425-3431. 10.1167/iovs.16-21377. Green open access

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Abstract

PURPOSE: The purpose of this study was to develop a topical matrix metalloproteinase inhibitor preparation for antiscarring therapy. METHODS: The broad spectrum matrix metalloproteinase inhibitor ilomastat was formulated using 2-hydroxypropyl-β-cyclodextrin in aqueous solution. In vitro activity of ilomastat-cyclodextrin (ilomastat-CD) was examined using fibroblasts seeded in collagen. Permeation of ilomastat-CD eye drop through pig eye conjunctiva was confirmed using Franz diffusion cells. Ilomastat-CD eye drop was applied to rabbit eyes in vivo, and the distribution of ilomastat in ocular tissues and fluids was determined by liquid chromatography-mass spectroscopy. RESULTS: The aqueous solubility of ilomastat-CD was ∼1000 μg/mL in water and 1400 μg/mL in PBS (pH 7.4), which is greater than ilomastat alone (140 and 160 μg/mL in water and PBS, respectively). The in vitro activity of ilomastat-CD to inhibit collagen contraction in the presence of human Tenon fibroblast cells was unchanged compared to uncomplexed ilomastat. Topically administered ilomastat-CD in vivo to rabbit eyes resulted in a therapeutic concentration of ilomastat being present in the sclera and conjunctiva and within the aqueous humor. CONCLUSIONS: Ilomastat-CD has the potential to be formulated as an eye drop for use as an antifibrotic, which may have implications for the prevention of scarring in many settings, for example glaucoma filtration surgery.

Type: Article
Title: An Ilomastat-CD Eye Drop Formulation to Treat Ocular Scarring
Location: United States
Open access status: An open access version is available from UCL Discovery
DOI: 10.1167/iovs.16-21377
Publisher version: http://doi.org/10.1167/iovs.16-21377
Language: English
Additional information: Copyright © 2017 The Authors. This work is licensed under a Creative Commons Attribution 4.0 International License (http://creativecommons.org/licenses/by/4.0). - Please note a correction to the Creative Commons licence was issued February 2018.
Keywords: ilomastat, antiscarring, ocular drug delivery, cyclodextrin, solubilization
UCL classification: UCL
UCL > Provost and Vice Provost Offices
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Brain Sciences
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Brain Sciences > Institute of Ophthalmology
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences > UCL School of Pharmacy
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences > UCL School of Pharmacy > Pharmaceutics
URI: https://discovery.ucl.ac.uk/id/eprint/1565022
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