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Short Term Stability Testing of Efavirenz-Loaded Solid Lipid Nanoparticle (SLN) and Nanostructured Lipid Carrier (NLC) Dispersions
Open AccessArticle

Design and Optimization of Nanostructured Lipid Carrier Containing Dexamethasone for Ophthalmic Use

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
Department of Cell Biology and Molecular Medicine, University of Szeged, Somogyi u. 4, H-6720 Szeged, Hungary
*
Author to whom correspondence should be addressed.
Pharmaceutics 2019, 11(12), 679; https://doi.org/10.3390/pharmaceutics11120679
Received: 4 October 2019 / Revised: 11 December 2019 / Accepted: 12 December 2019 / Published: 14 December 2019
(This article belongs to the Special Issue Advances in Solid Lipid Micro- and Nanoparticle Technology)
The aim of this study was to perform a preformulation study of dexamethasone (DXM)-loaded nanostructured lipid carriers (NLCs) for ocular use. Lipid screening was applied to find the most suitable solid and liquid lipids and surfactant for the NLC formulation. The visual observation was proved with XRD measurements for the establishment of the soluble state of DXM. Thermoanalytical measurements indicated that the most relevant depression of the crystallinity index could be ensured when using a 7:3 solid lipid:oil ratio. In order to optimize the NLC composition, a 23 full factorial experimental design was used. It was established that each independent factor (lipid, DXM, and surfactant concentration) had a significant effect on the particle size while in the case of entrapment efficiency, the DXM and surfactant concentrations were significant. Lower surfactant and lipid concentrations could be beneficial because the stability and the entrapment efficacy of NLCs were more favorable. The toxicity tests on human cornea cells indicated good ophthalmic tolerability of NLCs. The in vitro drug release study predicted a higher concentration of the solute DXM on the eye surface while the Raman mapping penetration study on the porcine cornea showed a high concentration of nanocarriers in the hydrophylic stroma layer. View Full-Text
Keywords: dexamethasone; nanostructured lipid carrier; factorial design; zeta potential; particle size; entrapment efficiency; human cornea cells toxicity; porcine cornea penetration; Raman mapping dexamethasone; nanostructured lipid carrier; factorial design; zeta potential; particle size; entrapment efficiency; human cornea cells toxicity; porcine cornea penetration; Raman mapping
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MDPI and ACS Style

L. Kiss, E.; Berkó, S.; Gácsi, A.; Kovács, A.; Katona, G.; Soós, J.; Csányi, E.; Gróf, I.; Harazin, A.; Deli, M.A.; Budai-Szűcs, M. Design and Optimization of Nanostructured Lipid Carrier Containing Dexamethasone for Ophthalmic Use. Pharmaceutics 2019, 11, 679.

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