Ocular Application of Oleuropein in Dry Eye Treatment: Formulation Studies and Biological Evaluation

Background. Oleuropein is already known for its numerous pharmacological properties, but its activity in the ocular field has not yet been investigated. The study aims to verify a possible use of oleuropein (OLE)-based eye drops both in terms of efficacy in dry eye syndrome and stability in aqueous...

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Autores principales:	Susi Burgalassi, Erica Zucchetti, Elena Birindelli, Silvia Tampucci, Patrizia Chetoni, Daniela Monti
Formato:	article
Lenguaje:	EN
Publicado:	MDPI AG 2021
Materias:	oleuropein dry eye syndrome liposomes stability hyperosmotic stress oxidative stress Medicine R Pharmacy and materia medica RS1-441
Acceso en línea:	https://doaj.org/article/ee6c44187a374a8785fee23af9810f4d
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spelling	oai:doaj.org-article:ee6c44187a374a8785fee23af9810f4d2021-11-25T18:39:45ZOcular Application of Oleuropein in Dry Eye Treatment: Formulation Studies and Biological Evaluation10.3390/ph141111511424-8247https://doaj.org/article/ee6c44187a374a8785fee23af9810f4d2021-11-01T00:00:00Zhttps://www.mdpi.com/1424-8247/14/11/1151https://doaj.org/toc/1424-8247Background. Oleuropein is already known for its numerous pharmacological properties, but its activity in the ocular field has not yet been investigated. The study aims to verify a possible use of oleuropein (OLE)-based eye drops both in terms of efficacy in dry eye syndrome and stability in aqueous solution. Methods. OLE was co-precipitated with HP-β-cyclodextrin, and the obtained complex was encapsulated into liposomes prepared by hydration of a lipid film composed of Lipoid S100 and cholesterol with different pH buffer solutions. The hydrated vesicles were shrunk by ultrasonication or extrusion. The preparations were characterized from the physicochemical point of view by subjecting them to differential scanning calorimetry, ATR-FTIR, dynamic light scattering analysis, and microscopy. Subsequently, OLE protective activity against hyperosmotic and oxidative stress on rabbit corneal epithelial cells (RCE) was evaluated. Results. The liposomal vesicles obtained after extrusion showed a tendency towards greater encapsulation efficiency (up to 80.77%) compared to that obtained by sonication, and the liposomes hydrated in pH 5.5 solution tended to incapsulate more than the neutral ones. Ultrasonication produced two-dimensional populations of liposomes, the largest of which reached 2149 nm. On the contrary, the extruded liposomes showed homogeneous diameters of about 250 nm. Complexation with cyclodextrin and subsequent encapsulation in liposomes greatly increased the OLE stability in aqueous solution, especially at 4 °C and for the extruded formulations. OLE aqueous solution (OLE7.4-sol, reference) and neutral extruded liposomes (F7.4-e) were well tolerated on RCE cells. Moreover, OLE was able to control the effects of hyperosmolarity on ocular surface cells and to prevent oxidative stress-induced loss of cell viability.Susi BurgalassiErica ZucchettiElena BirindelliSilvia TampucciPatrizia ChetoniDaniela MontiMDPI AGarticleoleuropeindry eye syndromeliposomesstabilityhyperosmotic stressoxidative stressMedicineRPharmacy and materia medicaRS1-441ENPharmaceuticals, Vol 14, Iss 1151, p 1151 (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	oleuropein dry eye syndrome liposomes stability hyperosmotic stress oxidative stress Medicine R Pharmacy and materia medica RS1-441
spellingShingle	oleuropein dry eye syndrome liposomes stability hyperosmotic stress oxidative stress Medicine R Pharmacy and materia medica RS1-441 Susi Burgalassi Erica Zucchetti Elena Birindelli Silvia Tampucci Patrizia Chetoni Daniela Monti Ocular Application of Oleuropein in Dry Eye Treatment: Formulation Studies and Biological Evaluation
description	Background. Oleuropein is already known for its numerous pharmacological properties, but its activity in the ocular field has not yet been investigated. The study aims to verify a possible use of oleuropein (OLE)-based eye drops both in terms of efficacy in dry eye syndrome and stability in aqueous solution. Methods. OLE was co-precipitated with HP-β-cyclodextrin, and the obtained complex was encapsulated into liposomes prepared by hydration of a lipid film composed of Lipoid S100 and cholesterol with different pH buffer solutions. The hydrated vesicles were shrunk by ultrasonication or extrusion. The preparations were characterized from the physicochemical point of view by subjecting them to differential scanning calorimetry, ATR-FTIR, dynamic light scattering analysis, and microscopy. Subsequently, OLE protective activity against hyperosmotic and oxidative stress on rabbit corneal epithelial cells (RCE) was evaluated. Results. The liposomal vesicles obtained after extrusion showed a tendency towards greater encapsulation efficiency (up to 80.77%) compared to that obtained by sonication, and the liposomes hydrated in pH 5.5 solution tended to incapsulate more than the neutral ones. Ultrasonication produced two-dimensional populations of liposomes, the largest of which reached 2149 nm. On the contrary, the extruded liposomes showed homogeneous diameters of about 250 nm. Complexation with cyclodextrin and subsequent encapsulation in liposomes greatly increased the OLE stability in aqueous solution, especially at 4 °C and for the extruded formulations. OLE aqueous solution (OLE7.4-sol, reference) and neutral extruded liposomes (F7.4-e) were well tolerated on RCE cells. Moreover, OLE was able to control the effects of hyperosmolarity on ocular surface cells and to prevent oxidative stress-induced loss of cell viability.
format	article
author	Susi Burgalassi Erica Zucchetti Elena Birindelli Silvia Tampucci Patrizia Chetoni Daniela Monti
author_facet	Susi Burgalassi Erica Zucchetti Elena Birindelli Silvia Tampucci Patrizia Chetoni Daniela Monti
author_sort	Susi Burgalassi
title	Ocular Application of Oleuropein in Dry Eye Treatment: Formulation Studies and Biological Evaluation
title_short	Ocular Application of Oleuropein in Dry Eye Treatment: Formulation Studies and Biological Evaluation
title_full	Ocular Application of Oleuropein in Dry Eye Treatment: Formulation Studies and Biological Evaluation
title_fullStr	Ocular Application of Oleuropein in Dry Eye Treatment: Formulation Studies and Biological Evaluation
title_full_unstemmed	Ocular Application of Oleuropein in Dry Eye Treatment: Formulation Studies and Biological Evaluation
title_sort	ocular application of oleuropein in dry eye treatment: formulation studies and biological evaluation
publisher	MDPI AG
publishDate	2021
url	https://doaj.org/article/ee6c44187a374a8785fee23af9810f4d
work_keys_str_mv	AT susiburgalassi ocularapplicationofoleuropeinindryeyetreatmentformulationstudiesandbiologicalevaluation AT ericazucchetti ocularapplicationofoleuropeinindryeyetreatmentformulationstudiesandbiologicalevaluation AT elenabirindelli ocularapplicationofoleuropeinindryeyetreatmentformulationstudiesandbiologicalevaluation AT silviatampucci ocularapplicationofoleuropeinindryeyetreatmentformulationstudiesandbiologicalevaluation AT patriziachetoni ocularapplicationofoleuropeinindryeyetreatmentformulationstudiesandbiologicalevaluation AT danielamonti ocularapplicationofoleuropeinindryeyetreatmentformulationstudiesandbiologicalevaluation
_version_	1718410869365276672

Ocular Application of Oleuropein in Dry Eye Treatment: Formulation Studies and Biological Evaluation

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