Functional ibuprofen-loaded cationic nanoemulsion: Development and optimization for dry eye disease treatment
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2020
Authors
Jurišić Dukovski, BiseraJuretić, Marina
Bračko, Danka
Randjelović, Danijela
Savić, Snežana

Crespo Moral, Mario
Diebold, Yolanda
Filipović-Grčić, Jelena
Grigorov, Ivan
Lovrić, Jasmina
Article (Published version)

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Inflammation plays a key role in dry eye disease (DED) affecting millions of people worldwide. Non-steroidal anti-inflammatory drugs (NSAIDs) can be used topically to act on the inflammatory component of DED, but their limited aqueous solubility raises formulation issues. The aim of this study was development and optimization of functional cationic nanoemulsions (NEs) for DED treatment, as a formulation approach to circumvent solubility problems, prolong drug residence at the ocular surface and stabilize the tear film. Ibuprofen was employed as the model NSAID, chitosan as the cationic agent, and lecithin as the anionic surfactant enabling chitosan incorporation. Moreover, lecithin is a mixture of phospholipids including phosphatidylcholine and phosphatidylethanolamine, two constituents of the natural tear film important for its stability. NEs were characterized in terms of droplet size, polydispersity index, zeta-potential, pH, viscosity, osmolarity, surface tension, entrapment effici...ency, stability, sterilizability and in vitro release. NEs mucoadhesive properties were tested rheologically after mixing with mucin dispersion. Biocompatibility was assessed employing 3D HCE-T cell-based model and ex vivo model using porcine corneas. The results of our study pointed out the NE formulation with 0.05% (w/w) chitosan as the lead formulation with physicochemical properties adequate for ophthalmic application, mucoadhesive character and excellent biocompatibility.
Keywords:
Chitosan / Dry eye disease / Lecithin / Nanoemulsion / NSAIDSource:
International Journal of Pharmaceutics, 2020, 576Publisher:
- Elsevier B.V.
Funding / projects:
- Topical nanodelivery systems funded by the University of Zagreb (Z169), the project “Modelling of the Pharmaceutical Spray Drying Process of the Emulsions in Laboratory and Pilot Scale” in collaboration with the industrial partner PLIVA Croatia Ltd.
- Spanish Government Grant RTI2018-094071-B-C21 (MCIU/AEI/FEDER, UE) (YD and MC-M).
DOI: 10.1016/j.ijpharm.2019.118979
ISSN: 0378-5173
WoS: 000512972500015
Scopus: 2-s2.0-85077471068
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PharmacyTY - JOUR AU - Jurišić Dukovski, Bisera AU - Juretić, Marina AU - Bračko, Danka AU - Randjelović, Danijela AU - Savić, Snežana AU - Crespo Moral, Mario AU - Diebold, Yolanda AU - Filipović-Grčić, Jelena AU - Grigorov, Ivan AU - Lovrić, Jasmina PY - 2020 UR - https://farfar.pharmacy.bg.ac.rs/handle/123456789/3523 AB - Inflammation plays a key role in dry eye disease (DED) affecting millions of people worldwide. Non-steroidal anti-inflammatory drugs (NSAIDs) can be used topically to act on the inflammatory component of DED, but their limited aqueous solubility raises formulation issues. The aim of this study was development and optimization of functional cationic nanoemulsions (NEs) for DED treatment, as a formulation approach to circumvent solubility problems, prolong drug residence at the ocular surface and stabilize the tear film. Ibuprofen was employed as the model NSAID, chitosan as the cationic agent, and lecithin as the anionic surfactant enabling chitosan incorporation. Moreover, lecithin is a mixture of phospholipids including phosphatidylcholine and phosphatidylethanolamine, two constituents of the natural tear film important for its stability. NEs were characterized in terms of droplet size, polydispersity index, zeta-potential, pH, viscosity, osmolarity, surface tension, entrapment efficiency, stability, sterilizability and in vitro release. NEs mucoadhesive properties were tested rheologically after mixing with mucin dispersion. Biocompatibility was assessed employing 3D HCE-T cell-based model and ex vivo model using porcine corneas. The results of our study pointed out the NE formulation with 0.05% (w/w) chitosan as the lead formulation with physicochemical properties adequate for ophthalmic application, mucoadhesive character and excellent biocompatibility. PB - Elsevier B.V. T2 - International Journal of Pharmaceutics T1 - Functional ibuprofen-loaded cationic nanoemulsion: Development and optimization for dry eye disease treatment VL - 576 DO - 10.1016/j.ijpharm.2019.118979 ER -
@article{ author = "Jurišić Dukovski, Bisera and Juretić, Marina and Bračko, Danka and Randjelović, Danijela and Savić, Snežana and Crespo Moral, Mario and Diebold, Yolanda and Filipović-Grčić, Jelena and Grigorov, Ivan and Lovrić, Jasmina", year = "2020", abstract = "Inflammation plays a key role in dry eye disease (DED) affecting millions of people worldwide. Non-steroidal anti-inflammatory drugs (NSAIDs) can be used topically to act on the inflammatory component of DED, but their limited aqueous solubility raises formulation issues. The aim of this study was development and optimization of functional cationic nanoemulsions (NEs) for DED treatment, as a formulation approach to circumvent solubility problems, prolong drug residence at the ocular surface and stabilize the tear film. Ibuprofen was employed as the model NSAID, chitosan as the cationic agent, and lecithin as the anionic surfactant enabling chitosan incorporation. Moreover, lecithin is a mixture of phospholipids including phosphatidylcholine and phosphatidylethanolamine, two constituents of the natural tear film important for its stability. NEs were characterized in terms of droplet size, polydispersity index, zeta-potential, pH, viscosity, osmolarity, surface tension, entrapment efficiency, stability, sterilizability and in vitro release. NEs mucoadhesive properties were tested rheologically after mixing with mucin dispersion. Biocompatibility was assessed employing 3D HCE-T cell-based model and ex vivo model using porcine corneas. The results of our study pointed out the NE formulation with 0.05% (w/w) chitosan as the lead formulation with physicochemical properties adequate for ophthalmic application, mucoadhesive character and excellent biocompatibility.", publisher = "Elsevier B.V.", journal = "International Journal of Pharmaceutics", title = "Functional ibuprofen-loaded cationic nanoemulsion: Development and optimization for dry eye disease treatment", volume = "576", doi = "10.1016/j.ijpharm.2019.118979" }
Jurišić Dukovski, B., Juretić, M., Bračko, D., Randjelović, D., Savić, S., Crespo Moral, M., Diebold, Y., Filipović-Grčić, J., Grigorov, I.,& Lovrić, J.. (2020). Functional ibuprofen-loaded cationic nanoemulsion: Development and optimization for dry eye disease treatment. in International Journal of Pharmaceutics Elsevier B.V.., 576. https://doi.org/10.1016/j.ijpharm.2019.118979
Jurišić Dukovski B, Juretić M, Bračko D, Randjelović D, Savić S, Crespo Moral M, Diebold Y, Filipović-Grčić J, Grigorov I, Lovrić J. Functional ibuprofen-loaded cationic nanoemulsion: Development and optimization for dry eye disease treatment. in International Journal of Pharmaceutics. 2020;576. doi:10.1016/j.ijpharm.2019.118979 .
Jurišić Dukovski, Bisera, Juretić, Marina, Bračko, Danka, Randjelović, Danijela, Savić, Snežana, Crespo Moral, Mario, Diebold, Yolanda, Filipović-Grčić, Jelena, Grigorov, Ivan, Lovrić, Jasmina, "Functional ibuprofen-loaded cationic nanoemulsion: Development and optimization for dry eye disease treatment" in International Journal of Pharmaceutics, 576 (2020), https://doi.org/10.1016/j.ijpharm.2019.118979 . .