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Int. J. Mol. Sci. 2017, 18(10), 2076; doi:10.3390/ijms18102076

Topical Ocular Delivery of TGF-β1 to the Back of the Eye: Implications in Age-Related Neurodegenerative Diseases

1
Section of Pharmacology, Department of Biomedical and Biotechnological Sciences, School of Medicine, University of Catania, 95123 Catania, Italy
2
Center for Research in Ocular Pharmacology—CERFO University of Catania, 95123 Catania, Italy
3
Department of Drug Sciences, University of Catania, 95125 Catania, Italy
4
NANO-i—Research Center on Ocular Nanotechnology, University of Catania, 95125 Catania, Italy
5
IRCSS Associazione Oasi Maria S.S., Institute for Research on Mental Retardation and Brain Aging, 94018 Troina, Italy
These authors have equally supervised this work.
*
Author to whom correspondence should be addressed.
Received: 28 August 2017 / Revised: 22 September 2017 / Accepted: 27 September 2017 / Published: 30 September 2017
(This article belongs to the Special Issue Retinal Diseases: Bridging Basic and Clinical Research)
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Abstract

Dysregulation of the transforming growth factor-β1 (TGF-β1)/selected small mother against decapentaplegic (SMAD) pathway can be implicated in development of age-related macular degeneration (AMD), and the delivery of TGF-β1 could be beneficial for AMD. We developed a new ophthalmic formulation of TGF-β1 assessing the ocular pharmacokinetic profile of TGF-β1 in the rabbit eye. Small unilamellar vesicles (SUV) loaded with TGF-β1 were complemented with Annexin V and Ca2+, and the vitreous bioavailability of TGF-β1 was assessed after topical ocular administration by a commercial ELISA kit. We detected high levels of TGF-β1 (Cmax 114.7 ± 12.40 pg/mL) in the vitreous after 60 min (Tmax) from the topical application of the liposomal suspension. Ocular tolerability was also assessed by a modified Draize’s test. The new formulation was well tolerated. In conclusion, we demonstrated that the novel formulation was able to deliver remarkable levels of TGF-β1 into the back of the eye after topical administration. Indeed, this TGF-β1 delivery system may be useful in clinical practice to manage ophthalmic conditions such as age-related macular degeneration, skipping invasive intraocular injections. View Full-Text
Keywords: TGF-β1; age-related neurodegenerative diseases; retina; liposomes TGF-β1; age-related neurodegenerative diseases; retina; liposomes
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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Platania, C.B.M.; Fisichella, V.; Fidilio, A.; Geraci, F.; Lazzara, F.; Leggio, G.M.; Salomone, S.; Drago, F.; Pignatello, R.; Caraci, F.; Bucolo, C. Topical Ocular Delivery of TGF-β1 to the Back of the Eye: Implications in Age-Related Neurodegenerative Diseases. Int. J. Mol. Sci. 2017, 18, 2076.

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