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A pharmacokinetic study of a combination of beta adrenoreceptor antagonists : In the isolated perfused ovine eye

Mains, Jenifer and Tan, Lay Ean and Wilson, Clive and Urquhart, Andrew (2012) A pharmacokinetic study of a combination of beta adrenoreceptor antagonists : In the isolated perfused ovine eye. European Journal of Pharmaceutics and Biopharmaceutics, 80 (2). pp. 393-401. ISSN 0939-6411

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Abstract

The treatment of posterior eye diseases, such as diabetic retinopathy and age-related macular degeneration, is of growing interest as the number of people affected by these conditions continues to rise. This study utilises the methods of cassette dosing and the perfused ovine eye model – to reduce animal usage and therefore animal time – to show that for a series of beta adrenoreceptor antagonists, lipophilicity is a key physicochemical property that governs drug distribution within the eye. Following intravitreal injection, lipophilic beta adrenoreceptor antagonists penetrate to the posterior eye, where they bind to the choroid and reside in the retina at greater concentrations than more hydrophilic beta adrenoreceptor antagonists, which preferentially penetrate to the anterior eye.