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

Research output: Contribution to journalArticle

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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.

Original languageEnglish
Article number2076
JournalInternational Journal of Molecular Sciences
Volume18
Issue number10
DOIs
Publication statusPublished - Oct 1 2017

Fingerprint

Neurodegenerative diseases
Transforming Growth Factors
Neurodegenerative Diseases
delivery
degeneration
Macular Degeneration
Topical Administration
formulations
Ophthalmic Administration
Intraocular Injections
Intercellular Signaling Peptides and Proteins
bioavailability
Unilamellar Liposomes
kits
Pharmacokinetics
Annexin A5
rabbits
Biological Availability
Suspensions
Enzyme-Linked Immunosorbent Assay

Keywords

  • Age-related neurodegenerative diseases
  • Liposomes
  • Retina
  • TGF-β1

ASJC Scopus subject areas

  • Catalysis
  • Molecular Biology
  • Spectroscopy
  • Computer Science Applications
  • Physical and Theoretical Chemistry
  • Organic Chemistry
  • Inorganic Chemistry

Cite this

Platania, C. B. M., Fisichella, V., Fidilio, A., Geraci, F., Lazzara, F., Leggio, G. M., ... Bucolo, C. (2017). Topical ocular delivery of TGF-β1 to the back of the eye: Implications in age-related neurodegenerative diseases. International Journal of Molecular Sciences, 18(10), [2076]. https://doi.org/10.3390/ijms18102076

Topical ocular delivery of TGF-β1 to the back of the eye : Implications in age-related neurodegenerative diseases. / Platania, Chiara Bianca Maria; Fisichella, Vincenzo; Fidilio, Annamaria; Geraci, Federica; Lazzara, Francesca; Leggio, Gian Marco; Salomone, Salvatore; Drago, Filippo; Pignatello, Rosario; Caraci, Filippo; Bucolo, Claudio.

In: International Journal of Molecular Sciences, Vol. 18, No. 10, 2076, 01.10.2017.

Research output: Contribution to journalArticle

Platania, CBM, Fisichella, V, Fidilio, A, Geraci, F, Lazzara, F, Leggio, GM, Salomone, S, Drago, F, Pignatello, R, Caraci, F & Bucolo, C 2017, 'Topical ocular delivery of TGF-β1 to the back of the eye: Implications in age-related neurodegenerative diseases', International Journal of Molecular Sciences, vol. 18, no. 10, 2076. https://doi.org/10.3390/ijms18102076
Platania, Chiara Bianca Maria ; Fisichella, Vincenzo ; Fidilio, Annamaria ; Geraci, Federica ; Lazzara, Francesca ; Leggio, Gian Marco ; Salomone, Salvatore ; Drago, Filippo ; Pignatello, Rosario ; Caraci, Filippo ; Bucolo, Claudio. / Topical ocular delivery of TGF-β1 to the back of the eye : Implications in age-related neurodegenerative diseases. In: International Journal of Molecular Sciences. 2017 ; Vol. 18, No. 10.
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