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Predicting the biopharmaceutical properties of ibuprofen-loaded cationic nanoemulsion using 3D in vitro corneal model

INTRODUCTION Dry eye disease is a multifactorial disease of the ocular surface characterized by instability and increased osmolarity of the tear film, ocular surface inflammation and damage [1]. Current strategies are focused on the development of O/W nanoemulsions since their nanosized lipid dispersed phase can improve the tear film stability [2]. Moreover, cationic nanoemulsions bear the poteintial to increase both, precorneal drug residence time and corneal epithelium related absorption. Current project is focused on the development of ibuprofen- loaded cationic nanoemulsion optimized for its biocompatibility and therapeutic potential using 3D in vitro cell model. MATERIALS AND METHODS Nanoemulsions were produced using microfluidizer (Model M-110EH-30, Microfluidics, USA). The oil phase was composed of Mygliol 812, lecithin S45 and ibuprofen, and the aqueous phase of Cremophor EL, low molecular weight chitosan, glycerol and water. Nanoemulsions were characterized in terms of droplet size and zeta potential (Zetasizer 3000 HS, Malvern Instruments, UK), pH, osmolarity, in vitro release and stability. 3D in vitro model based on human corneal epithelial cells (HCE-T, Rikken, Japan) was used in biocompatibility, mucoadhesion and therapeutic potential screening. RESULTS Within this project, formulation and process parameters of nanoemulsion preparation have been optimized. Ibuprofen-loaded cationic ophthalmic nanoemulsions with droplet size of 163, 3 ± 0, 7 to 185, 0 ± 2, 1 nm, polydispersity index of 0, 11 ± 0, 02 to 0, 21 ± 0, 02 and zeta potential of 16, 4 ± 0, 6 to 36, 5 ± 1, 4 mV have been successfuly prepared. Chitosan coating was shown to provide pronounced mucoadhesivity while showing compatibility with 3D HCE-T cell model. CONCLUSION This study showed the potential of cationic nanoemulsions to be developed into a value- added delivery platform of ibuprofen for efficient symptomatic and causative dry eye disease treatment. REFERENCES [1] Craig J.P. et al. Ocul. Surf. 15, 276-283 (2017) [2] Gan L. et al. Drug Discov. Today 18, 290- 297 (2013)

nanoemulsions, ibuprofen, chitosan, HCE-T cells, mucoadhesion

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