Abstract: Inflammation plays a key role in dry eye disease (DED)affecting millions of people worldwide. Non-steroidal anti-inflammatorydrugs (NSAIDs) can be used topically to act on the inflammatory componentof DED, but their limited aqueous solubility raises formulation issues.The aim of this study was development and optimization of functionalcationic nanoemulsions (NEs) for DED treatment, as a formulation approachto circumvent solubility problems, prolong drug residence at the ocularsurface and stabilize the tear film. Ibuprofen was employed as the modelNSAID, chitosan as the cationic agent, and lecithin as the anionicsurfactant enabling chitosan incorporation. Moreover, lecithin is amixture of phospholipids including phosphatidylcholine andphosphatidylethanolamine, two constituents of the natural tear filmimportant for its stability. NEs were characterized in terms of dropletsize, polydispersity index, zeta-potential, pH, viscosity, osmolarity,surface tension, entrapment efficiency..., stability, sterilizability and invitro release. NEs mucoadhesive properties were tested rheologicallyafter mixing with mucin dispersion. Biocompatibility was assessedemploying 3D HCE-T cell-based model and ex vivo model using porcinecorneas. The results of our study pointed out the NE formulation with0.05 % (w/w) chitosan as the lead formulation with physicochemicalproperties adequate for ophthalmic application, mucoadhesive characterand excellent biocompatibility.
International Journal of Pharmaceutics, 2020, 576, 118979-
Publisher:
Elsevier BV
Funding / projects:
Spanish Government Grant RTI2018-094071-B-C21 (MCIU/AEI/FEDER, UE) (YD and MC-M)
opical nanodelivery systems funded by the University of Zagreb (Z169)
“Modelling of the Pharmaceutical Spray Drying Process of the Emulsions in Laboratory and Pilot Scale” in collaboration with the industrial partner PLIVA Croatia Ltd.
TY - 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 - Pepić, Ivan
AU - Lovrić, Jasmina
PY - 2020
UR - https://cer.ihtm.bg.ac.rs/handle/123456789/4012
AB - Abstract: Inflammation plays a key role in dry eye disease (DED)affecting millions of people worldwide. Non-steroidal anti-inflammatorydrugs (NSAIDs) can be used topically to act on the inflammatory componentof DED, but their limited aqueous solubility raises formulation issues.The aim of this study was development and optimization of functionalcationic nanoemulsions (NEs) for DED treatment, as a formulation approachto circumvent solubility problems, prolong drug residence at the ocularsurface and stabilize the tear film. Ibuprofen was employed as the modelNSAID, chitosan as the cationic agent, and lecithin as the anionicsurfactant enabling chitosan incorporation. Moreover, lecithin is amixture of phospholipids including phosphatidylcholine andphosphatidylethanolamine, two constituents of the natural tear filmimportant for its stability. NEs were characterized in terms of dropletsize, polydispersity index, zeta-potential, pH, viscosity, osmolarity,surface tension, entrapment efficiency, stability, sterilizability and invitro release. NEs mucoadhesive properties were tested rheologicallyafter mixing with mucin dispersion. Biocompatibility was assessedemploying 3D HCE-T cell-based model and ex vivo model using porcinecorneas. The results of our study pointed out the NE formulation with0.05 % (w/w) chitosan as the lead formulation with physicochemicalproperties adequate for ophthalmic application, mucoadhesive characterand excellent biocompatibility.
PB - Elsevier BV
T2 - International Journal of Pharmaceutics
T1 - Functional ibuprofen-loaded cationic nanoemulsion: Development and optimization for dry eye disease treatment
VL - 576
SP - 118979
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 Pepić, Ivan and Lovrić, Jasmina",
year = "2020",
abstract = "Abstract: Inflammation plays a key role in dry eye disease (DED)affecting millions of people worldwide. Non-steroidal anti-inflammatorydrugs (NSAIDs) can be used topically to act on the inflammatory componentof DED, but their limited aqueous solubility raises formulation issues.The aim of this study was development and optimization of functionalcationic nanoemulsions (NEs) for DED treatment, as a formulation approachto circumvent solubility problems, prolong drug residence at the ocularsurface and stabilize the tear film. Ibuprofen was employed as the modelNSAID, chitosan as the cationic agent, and lecithin as the anionicsurfactant enabling chitosan incorporation. Moreover, lecithin is amixture of phospholipids including phosphatidylcholine andphosphatidylethanolamine, two constituents of the natural tear filmimportant for its stability. NEs were characterized in terms of dropletsize, polydispersity index, zeta-potential, pH, viscosity, osmolarity,surface tension, entrapment efficiency, stability, sterilizability and invitro release. NEs mucoadhesive properties were tested rheologicallyafter mixing with mucin dispersion. Biocompatibility was assessedemploying 3D HCE-T cell-based model and ex vivo model using porcinecorneas. The results of our study pointed out the NE formulation with0.05 % (w/w) chitosan as the lead formulation with physicochemicalproperties adequate for ophthalmic application, mucoadhesive characterand excellent biocompatibility.",
publisher = "Elsevier BV",
journal = "International Journal of Pharmaceutics",
title = "Functional ibuprofen-loaded cationic nanoemulsion: Development and optimization for dry eye disease treatment",
volume = "576",
pages = "118979",
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., Pepić, I.,& Lovrić, J.. (2020). Functional ibuprofen-loaded cationic nanoemulsion: Development and optimization for dry eye disease treatment. in International Journal of Pharmaceutics
Elsevier BV., 576, 118979.
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, Pepić I, Lovrić J. Functional ibuprofen-loaded cationic nanoemulsion: Development and optimization for dry eye disease treatment. in International Journal of Pharmaceutics. 2020;576:118979.
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, Pepić, Ivan, Lovrić, Jasmina, "Functional ibuprofen-loaded cationic nanoemulsion: Development and optimization for dry eye disease treatment" in International Journal of Pharmaceutics, 576 (2020):118979,
https://doi.org/10.1016/j.ijpharm.2019.118979 . .
