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

Chiara Bianca Maria Platania; Vincenzo Fisichella; Annamaria Fidilio; Federica Geraci; Francesca Lazzara; Gian Marco Leggio; Salvatore Salomone; Filippo Drago; Rosario Pignatello; Filippo Caraci; Claudio Bucolo

doi:10.3390/ijms18102076

International Journal of Molecular Sciences (Sep 2017)

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

Chiara Bianca Maria Platania,
Vincenzo Fisichella,
Annamaria Fidilio,
Federica Geraci,
Francesca Lazzara,
Gian Marco Leggio,
Salvatore Salomone,
Filippo Drago,
Rosario Pignatello,
Filippo Caraci,
Claudio Bucolo

Affiliations

Chiara Bianca Maria Platania: Section of Pharmacology, Department of Biomedical and Biotechnological Sciences, School of Medicine, University of Catania, 95123 Catania, Italy
Vincenzo Fisichella: Section of Pharmacology, Department of Biomedical and Biotechnological Sciences, School of Medicine, University of Catania, 95123 Catania, Italy
Annamaria Fidilio: Section of Pharmacology, Department of Biomedical and Biotechnological Sciences, School of Medicine, University of Catania, 95123 Catania, Italy
Federica Geraci: Section of Pharmacology, Department of Biomedical and Biotechnological Sciences, School of Medicine, University of Catania, 95123 Catania, Italy
Francesca Lazzara: Section of Pharmacology, Department of Biomedical and Biotechnological Sciences, School of Medicine, University of Catania, 95123 Catania, Italy
Gian Marco Leggio: Section of Pharmacology, Department of Biomedical and Biotechnological Sciences, School of Medicine, University of Catania, 95123 Catania, Italy
Salvatore Salomone: Section of Pharmacology, Department of Biomedical and Biotechnological Sciences, School of Medicine, University of Catania, 95123 Catania, Italy
Filippo Drago: Section of Pharmacology, Department of Biomedical and Biotechnological Sciences, School of Medicine, University of Catania, 95123 Catania, Italy
Rosario Pignatello: Center for Research in Ocular Pharmacology—CERFO University of Catania, 95123 Catania, Italy
Filippo Caraci: Department of Drug Sciences, University of Catania, 95125 Catania, Italy
Claudio Bucolo: Section of Pharmacology, Department of Biomedical and Biotechnological Sciences, School of Medicine, University of Catania, 95123 Catania, Italy

DOI: https://doi.org/10.3390/ijms18102076
Journal volume & issue: Vol. 18, no. 10
p. 2076

Abstract

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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.

Published in International Journal of Molecular Sciences

ISSN: 1661-6596 (Print); 1422-0067 (Online)
Publisher: MDPI AG
Country of publisher: Switzerland
LCC subjects: Science: Biology (General); Science: Chemistry
Website: http://www.mdpi.com/journal/ijms

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