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Volume 12
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10.3390/pharmaceutics12070682
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Article

Development and Characterization of Potential Ocular Mucoadhesive Nano Lipid Carriers Using Full Factorial Design

by
Eszter L. Kiss
1,
Szilvia Berkó
1,
Attila Gácsi
1,
Anita Kovács
1,
Gábor Katona
1,
Judit Soós
2,
Erzsébet Csányi
1,
Ilona Gróf
3,4,
András Harazin
3,
Mária A. Deli
3,
György T. Balogh
5,6 and
Mária Budai-Szűcs
1,*
1
Institute of Pharmaceutical Technology and Regulatory Affairs, Faculty of Pharmacy, University of Szeged, Eötvös u. 6, H-6720 Szeged, Hungary
2
Department of Ophthalmology, Faculty of Medicine, University of Szeged, Korányi Fasor 10-11, H-6720 Szeged, Hungary
3
Institute of Biophysics, Biological Research Centre, Temesvári krt. 62, H-6726 Szeged, Hungary
4
Doctoral School of Biology, University of Szeged, Dugonics tér 13, H-6720 Szeged, Hungary
5
Institute of Pharmacodynamics and Biopharmacy, Faculty of Pharmacy, University of Szeged, Eötvös u. 6, H-6720 Szeged, Hungary
6
Department of Chemical and Environmental Process Engineering, Budapest University of Technology and Economics, Műegyetem rakpart 3, 1111 Budapest, Hungary
*
Author to whom correspondence should be addressed.
Pharmaceutics 2020, 12(7), 682; https://doi.org/10.3390/pharmaceutics12070682
Submission received: 12 June 2020 / Revised: 14 July 2020 / Accepted: 15 July 2020 / Published: 20 July 2020
(This article belongs to the Special Issue Mucoadhesive and Mucosal Drug Delivery Systems)
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Abstract

Generally, topically applied eye drops have low bioavailability due to short residence time and low penetration of the drug. The aim of the present study was to incorporate dexamethasone (DXM) into nano lipid carriers (NLC), which contain mucoadhesive polymer, in order to increase the bioavailability of the drug. A 23 factorial experimental design was applied, in which the three factors were the polymer, the DXM, and the emulsifier concentrations. The samples were analyzed for particle size, zeta potential, polydispersity index, and Span value. The significant factors were identified. The biocompatibility of the formulations was evaluated with human corneal toxicity tests and immunoassay analysis. The possible increase in bioavailability was analyzed by means of mucoadhesivity, in vitro drug diffusion, and different penetration tests, such as in vitro cornea PAMPA model, human corneal cell penetration, and ex vivo porcine corneal penetration using Raman mapping. The results indicated that DXM can be incorporated in stable mucoadhesive NLC systems, which are non-toxic and do not have any harmful effect on cell junctions. Mucoadhesive NLCs can create a depot on the surface of the cornea, which can predict improved bioavailability.
Keywords: nano lipid carrier; mucoadhesion; immunoassay; cell toxicity; cornea PAMPA; penetration studies; Raman mapping nano lipid carrier; mucoadhesion; immunoassay; cell toxicity; cornea PAMPA; penetration studies; Raman mapping
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MDPI and ACS Style

Kiss, E.L.; Berkó, S.; Gácsi, A.; Kovács, A.; Katona, G.; Soós, J.; Csányi, E.; Gróf, I.; Harazin, A.; Deli, M.A.; et al. Development and Characterization of Potential Ocular Mucoadhesive Nano Lipid Carriers Using Full Factorial Design. Pharmaceutics 2020, 12, 682. https://doi.org/10.3390/pharmaceutics12070682

AMA Style

Kiss EL, Berkó S, Gácsi A, Kovács A, Katona G, Soós J, Csányi E, Gróf I, Harazin A, Deli MA, et al. Development and Characterization of Potential Ocular Mucoadhesive Nano Lipid Carriers Using Full Factorial Design. Pharmaceutics. 2020; 12(7):682. https://doi.org/10.3390/pharmaceutics12070682

Chicago/Turabian Style

Kiss, Eszter L., Szilvia Berkó, Attila Gácsi, Anita Kovács, Gábor Katona, Judit Soós, Erzsébet Csányi, Ilona Gróf, András Harazin, Mária A. Deli, and et al. 2020. "Development and Characterization of Potential Ocular Mucoadhesive Nano Lipid Carriers Using Full Factorial Design" Pharmaceutics 12, no. 7: 682. https://doi.org/10.3390/pharmaceutics12070682

APA Style

Kiss, E. L., Berkó, S., Gácsi, A., Kovács, A., Katona, G., Soós, J., Csányi, E., Gróf, I., Harazin, A., Deli, M. A., Balogh, G. T., & Budai-Szűcs, M. (2020). Development and Characterization of Potential Ocular Mucoadhesive Nano Lipid Carriers Using Full Factorial Design. Pharmaceutics, 12(7), 682. https://doi.org/10.3390/pharmaceutics12070682

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