Development of a non-settling gel formulation of 0.5% loteprednol etabonate for anti-inflammatory use as an ophthalmic drop

Martin J Coffey,1 Heleen H DeCory,2 Stephen S Lane31Pharmaceutical Product Development, Bausch and Lomb, Inc, Rochester, NY, USA; 2Global Medical Affairs, Pharmaceuticals, Bausch and Lomb, Inc, Rochester, NY, USA; 3Associated Eye Care, Stillwater, MN, USAAbstract: The eye has protective barriers (ie...

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Autores principales:	Coffey MJ, DeCory HH, Lane SS
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2013
Materias:	Ophthalmology RE1-994
Acceso en línea:	https://doaj.org/article/5bf698ef283d4c42ac60be0a97a3d826
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spelling	oai:doaj.org-article:5bf698ef283d4c42ac60be0a97a3d8262021-12-02T03:40:30ZDevelopment of a non-settling gel formulation of 0.5% loteprednol etabonate for anti-inflammatory use as an ophthalmic drop1177-54671177-5483https://doaj.org/article/5bf698ef283d4c42ac60be0a97a3d8262013-02-01T00:00:00Zhttp://www.dovepress.com/development-of-a-non-settling-gel-formulation-of-05-loteprednol-etabon-a12201https://doaj.org/toc/1177-5467https://doaj.org/toc/1177-5483Martin J Coffey,1 Heleen H DeCory,2 Stephen S Lane31Pharmaceutical Product Development, Bausch and Lomb, Inc, Rochester, NY, USA; 2Global Medical Affairs, Pharmaceuticals, Bausch and Lomb, Inc, Rochester, NY, USA; 3Associated Eye Care, Stillwater, MN, USAAbstract: The eye has protective barriers (ie, the conjunctival and corneal membranes) and defense mechanisms (ie, reflex tearing, blinking, lacrimal drainage) which present challenges to topical drug delivery. Topical ocular corticosteroids are commonly used in the treatment of anterior segment diseases and inflammation associated with ocular surgery, and manufacturers continually strive to improve their characteristics. We describe the development of a novel ophthalmic gel formulation of loteprednol etabonate (LE), a C-20 ester-based corticosteroid with an established safety profile, in the treatment of ocular inflammatory conditions. The new LE gel formulation is non-settling, eliminating the need to shake the product to resuspend the drug, has a pH close to that of tears, and a low preservative concentration. The rheological characteristics of LE gel are such that the formulation is instilled as a drop and transitions to a fluid upon instillation in the eye, yet retains sufficient viscosity to prolong ocular surface retention. The new formulation provides consistent, uniform dosing as evidenced by dose extrusion studies, while pharmacokinetic studies in rabbits demonstrated rapid and sustained exposure to LE in ocular tissues following instillation of LE gel. Finally, results from two clinical studies of LE gel in the treatment of postoperative inflammation and pain following cataract surgery indicate that it was safe and effective. Most patients reported no unpleasant drop sensation upon instillation, and reports of blurred vision were rare.Keywords: loteprednol etabonate, gel, drug delivery, clinical trial, ocular surfaceCoffey MJDeCory HHLane SSDove Medical PressarticleOphthalmologyRE1-994ENClinical Ophthalmology, Vol 2013, Iss default, Pp 299-312 (2013)
institution	DOAJ
collection	DOAJ
language	EN
topic	Ophthalmology RE1-994
spellingShingle	Ophthalmology RE1-994 Coffey MJ DeCory HH Lane SS Development of a non-settling gel formulation of 0.5% loteprednol etabonate for anti-inflammatory use as an ophthalmic drop
description	Martin J Coffey,1 Heleen H DeCory,2 Stephen S Lane31Pharmaceutical Product Development, Bausch and Lomb, Inc, Rochester, NY, USA; 2Global Medical Affairs, Pharmaceuticals, Bausch and Lomb, Inc, Rochester, NY, USA; 3Associated Eye Care, Stillwater, MN, USAAbstract: The eye has protective barriers (ie, the conjunctival and corneal membranes) and defense mechanisms (ie, reflex tearing, blinking, lacrimal drainage) which present challenges to topical drug delivery. Topical ocular corticosteroids are commonly used in the treatment of anterior segment diseases and inflammation associated with ocular surgery, and manufacturers continually strive to improve their characteristics. We describe the development of a novel ophthalmic gel formulation of loteprednol etabonate (LE), a C-20 ester-based corticosteroid with an established safety profile, in the treatment of ocular inflammatory conditions. The new LE gel formulation is non-settling, eliminating the need to shake the product to resuspend the drug, has a pH close to that of tears, and a low preservative concentration. The rheological characteristics of LE gel are such that the formulation is instilled as a drop and transitions to a fluid upon instillation in the eye, yet retains sufficient viscosity to prolong ocular surface retention. The new formulation provides consistent, uniform dosing as evidenced by dose extrusion studies, while pharmacokinetic studies in rabbits demonstrated rapid and sustained exposure to LE in ocular tissues following instillation of LE gel. Finally, results from two clinical studies of LE gel in the treatment of postoperative inflammation and pain following cataract surgery indicate that it was safe and effective. Most patients reported no unpleasant drop sensation upon instillation, and reports of blurred vision were rare.Keywords: loteprednol etabonate, gel, drug delivery, clinical trial, ocular surface
format	article
author	Coffey MJ DeCory HH Lane SS
author_facet	Coffey MJ DeCory HH Lane SS
author_sort	Coffey MJ
title	Development of a non-settling gel formulation of 0.5% loteprednol etabonate for anti-inflammatory use as an ophthalmic drop
title_short	Development of a non-settling gel formulation of 0.5% loteprednol etabonate for anti-inflammatory use as an ophthalmic drop
title_full	Development of a non-settling gel formulation of 0.5% loteprednol etabonate for anti-inflammatory use as an ophthalmic drop
title_fullStr	Development of a non-settling gel formulation of 0.5% loteprednol etabonate for anti-inflammatory use as an ophthalmic drop
title_full_unstemmed	Development of a non-settling gel formulation of 0.5% loteprednol etabonate for anti-inflammatory use as an ophthalmic drop
title_sort	development of a non-settling gel formulation of 0.5% loteprednol etabonate for anti-inflammatory use as an ophthalmic drop
publisher	Dove Medical Press
publishDate	2013
url	https://doaj.org/article/5bf698ef283d4c42ac60be0a97a3d826
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Development of a non-settling gel formulation of 0.5% loteprednol etabonate for anti-inflammatory use as an ophthalmic drop

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