Functional ibuprofen-loaded cationic nanoemulsion: Development and optimization for dry eye disease treatment
Authorized Users Only
AuthorsJurišić Dukovski, Bisera
Crespo Moral, Mario
Article (Published version)
MetadataShow full item record
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.
Keywords:dry eye disease / nanoemulsion / NSAID / chitosan / lecithin
Source:International Journal of Pharmaceutics, 2020, 576, 118979-
- Elsevier BV
- 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.
- The peer-reviewed version: https://cer.ihtm.bg.ac.rs/handle/123456789/4011