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Open AccessArticle

Dexamethasone Loaded Liposomes by Thin-Film Hydration and Microfluidic Procedures: Formulation Challenges

Department of Pharmaceutical and Pharmacological Sciences, University of Padova, Via F. Marzolo 5, 35131 Padova, Italy
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Author to whom correspondence should be addressed.
Int. J. Mol. Sci. 2020, 21(5), 1611; https://doi.org/10.3390/ijms21051611
Received: 4 February 2020 / Revised: 22 February 2020 / Accepted: 23 February 2020 / Published: 26 February 2020
Liposomes have been one of the most exploited drug delivery systems in recent decades. However, their large-scale production with low batch-to-batch differences is a challenge for industry, which ultimately delays the clinical translation of new products. We have investigated the effects of formulation parameters on the colloidal and biopharmaceutical properties of liposomes generated with a thin-film hydration approach and microfluidic procedure. Dexamethasone hemisuccinate was remotely loaded into liposomes using a calcium acetate gradient. The liposomes produced by microfluidic techniques showed a unilamellar structure, while the liposomes produced by thin-film hydration were multilamellar. Under the same remote loading conditions, a higher loading capacity and efficiency were observed for the liposomes obtained by microfluidics, with low batch-to-batch differences. Both formulations released the drug for almost one month with the liposomes prepared by microfluidics showing a slightly higher drug release in the first two days. This behavior was ascribed to the different structure of the two liposome formulations. In vitro studies showed that both formulations are non-toxic, associate to human Adult Retinal Pigment Epithelial cell line-19 (ARPE-19) cells, and efficiently reduce inflammation, with the liposomes obtained by the microfluidic technique slightly outperforming. The results demonstrated that the microfluidic technique offers advantages to generate liposomal formulations for drug-controlled release with an enhanced biopharmaceutical profile and with scalability. View Full-Text
Keywords: liposome formulation; microfluidic technique; dexamethasone loaded liposomes; controlled release liposome formulation; microfluidic technique; dexamethasone loaded liposomes; controlled release
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MDPI and ACS Style

Al-Amin, M.; Bellato, F.; Mastrotto, F.; Garofalo, M.; Malfanti, A.; Salmaso, S.; Caliceti, P. Dexamethasone Loaded Liposomes by Thin-Film Hydration and Microfluidic Procedures: Formulation Challenges. Int. J. Mol. Sci. 2020, 21, 1611. https://doi.org/10.3390/ijms21051611

AMA Style

Al-Amin M, Bellato F, Mastrotto F, Garofalo M, Malfanti A, Salmaso S, Caliceti P. Dexamethasone Loaded Liposomes by Thin-Film Hydration and Microfluidic Procedures: Formulation Challenges. International Journal of Molecular Sciences. 2020; 21(5):1611. https://doi.org/10.3390/ijms21051611

Chicago/Turabian Style

Al-Amin, MD; Bellato, Federica; Mastrotto, Francesca; Garofalo, Mariangela; Malfanti, Alessio; Salmaso, Stefano; Caliceti, Paolo. 2020. "Dexamethasone Loaded Liposomes by Thin-Film Hydration and Microfluidic Procedures: Formulation Challenges" Int. J. Mol. Sci. 21, no. 5: 1611. https://doi.org/10.3390/ijms21051611

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