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Robust Oil-core Nanocapsules with Hyaluronate-based Shells as Promising NanoVehicles for Lipophilic Compounds

Abstract

Designing of nanodelivery systems has been recently considered as a solution to the major challenge in pharmaceutical research - poor bioavailability of lipophilic drugs. Nanocapsules with liquid oil cores and shells based on amphiphilic polysaccharides were developed here as robust carriers of hydrophobic active compounds. A series of modified charged hyaluronates were synthesized and used as stabilizing shells ensuring also biocompatibility of the nanocapsules that is crucial for applications related to delivery of lipophilic drugs in vivo. Importantly, the oil nanodroplets were found to be stably suspended in water for at least 15 months without addition of low molar mass surfactants. Moreover, their size and stability may be tuned by varying the relative content of hydrophobic and hydrophilic groups in the hyaluronate derivatives as it was confirmed by dynamic light scattering, nanoparticle tracking analysis as well as electron microscopies. In vivo studies demonstrated that hyaluronate-based nanocapsules were accumulated preferentially in liver as well as in lungs. Moreover, their accumulation was dramatically potentiated in endotoxemic mice. In vitro studies showed that the nanocapsules were uptaken by Liver Sinusoidal Endothelial Cells and by Mouse Lung Vascular Endothelial Cells. Importantly, the capsules were found nontoxic in acute oral toxicity experiment even at a dose of 2000 mg/kg b.w. Biocompatible hyaluronate-based nanocapsules with liquid cores described herein represent a promissing and tunable nanodelivery system for lipophilic active compounds via both oral and intravenous administration.

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Publication details

The article was received on 08 Aug 2017, accepted on 04 Nov 2017 and first published on 06 Nov 2017


Article type: Paper
DOI: 10.1039/C7NR05851A
Citation: Nanoscale, 2017, Accepted Manuscript
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    Robust Oil-core Nanocapsules with Hyaluronate-based Shells as Promising NanoVehicles for Lipophilic Compounds

    J. Szafraniec, A. Blazejczyk, E. Maslak, M. Janik, G. Zając, J. Wietrzyk, S. Chlopicki and S. Zapotoczny, Nanoscale, 2017, Accepted Manuscript , DOI: 10.1039/C7NR05851A

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