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

Autor: Kiss EL; Institute of Pharmaceutical Technology and Regulatory Affairs, Faculty of Pharmacy, University of Szeged, Eötvös u. 6, H-6720 Szeged, Hungary., Berkó S; Institute of Pharmaceutical Technology and Regulatory Affairs, Faculty of Pharmacy, University of Szeged, Eötvös u. 6, H-6720 Szeged, Hungary., Gácsi A; Institute of Pharmaceutical Technology and Regulatory Affairs, Faculty of Pharmacy, University of Szeged, Eötvös u. 6, H-6720 Szeged, Hungary., Kovács A; Institute of Pharmaceutical Technology and Regulatory Affairs, Faculty of Pharmacy, University of Szeged, Eötvös u. 6, H-6720 Szeged, Hungary., Katona G; Institute of Pharmaceutical Technology and Regulatory Affairs, Faculty of Pharmacy, University of Szeged, Eötvös u. 6, H-6720 Szeged, Hungary., Soós J; Department of Ophthalmology, Faculty of Medicine, University of Szeged, Korányi Fasor 10-11, H-6720 Szeged, Hungary., Csányi E; Institute of Pharmaceutical Technology and Regulatory Affairs, Faculty of Pharmacy, University of Szeged, Eötvös u. 6, H-6720 Szeged, Hungary., Gróf I; Institute of Biophysics, Biological Research Centre, Temesvári krt. 62, H-6726 Szeged, Hungary.; Doctoral School of Biology, University of Szeged, Dugonics tér 13, H-6720 Szeged, Hungary., Harazin A; Institute of Biophysics, Biological Research Centre, Temesvári krt. 62, H-6726 Szeged, Hungary., Deli MA; Institute of Biophysics, Biological Research Centre, Temesvári krt. 62, H-6726 Szeged, Hungary., Balogh GT; Institute of Pharmacodynamics and Biopharmacy, Faculty of Pharmacy, University of Szeged, Eötvös u. 6, H-6720 Szeged, Hungary.; Department of Chemical and Environmental Process Engineering, Budapest University of Technology and Economics, Műegyetem rakpart 3, 1111 Budapest, Hungary., Budai-Szűcs M; Institute of Pharmaceutical Technology and Regulatory Affairs, Faculty of Pharmacy, University of Szeged, Eötvös u. 6, H-6720 Szeged, Hungary.
Jazyk: angličtina
Zdroj: Pharmaceutics [Pharmaceutics] 2020 Jul 20; Vol. 12 (7). Date of Electronic Publication: 2020 Jul 20.
DOI: 10.3390/pharmaceutics12070682
Abstrakt: 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 2 3 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.
Databáze: MEDLINE
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