Topical delivery of a Rho-kinase inhibitor to the cornea via mucoadhesive film

Chan, Wendy, Akhbanbetova, Alina, Quantock, Andrew J. ORCID: https://orcid.org/0000-0002-2484-3120 and Heard, Charles M. ORCID: https://orcid.org/0000-0001-9703-9777 2016. Topical delivery of a Rho-kinase inhibitor to the cornea via mucoadhesive film. European Journal of Pharmaceutical Sciences 91 , pp. 256-264. 10.1016/j.ejps.2016.05.016

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Abstract

The application of inhibitors of the Rho kinase pathway (ROCK inhibitors) to the surface of the eye in the form of eyedrops has beneficial effects which aid the recovery of diseased or injured endothelial cells that line the inner surface of the cornea. The aim of this study was to test the plausibility of delivering a selective ROCK inhibitor, Y-27,632, to the cornea using a thin polymeric film. Mucoadhesive polymeric thin films were prepared incorporating Y-27,632 and diffusional release into PBS was determined. Topical ocular delivery from the applied film was investigated using freshly excised porcine eyes and eyedrops of equivalent concentration acted as comparators; after 24 h the formulations were removed and the corneas extracted. Drug-loaded thin polymeric films, with high clarity and pliability were produced. ROCK inhibitor Y-27,632 was weakly retained within the film, with release attaining equilibrium after 1 h. This in turn facilitated its rapid ocular delivery, and an approximately three-fold greater penetration of Y-27,632 into cryoprobe-treated corneas was observed from the thin film (p < 0.01) compared to eyedrop. These findings support the further development of ROCK inhibitor delivery to the cornea via release from thin mucoadhesive films to treat vision loss cause by corneal endothelial dysfunction.

Item Type:	Article
Date Type:	Publication
Status:	Published
Schools:	Optometry and Vision Sciences Pharmacy
Subjects:	R Medicine > RE Ophthalmology
Publisher:	Elsevier
ISSN:	0928-0987
Date of First Compliant Deposit:	24 May 2016
Date of Acceptance:	14 May 2016
Last Modified:	03 May 2023 16:41
URI:	https://orca.cardiff.ac.uk/id/eprint/91212

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