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Hydrophobically-modified chitosan nanoliposomes for intestinal drug delivery

Zariwala, MG; Bendre, H; Markiv, A; Farnaud, S; Renshaw, D; Taylor, KMG; Somavarapu, S; (2018) Hydrophobically-modified chitosan nanoliposomes for intestinal drug delivery. International Journal of Nanomedicine , 13 pp. 5837-5848. 10.2147/IJN.S166901. Green open access

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Abstract

BACKGROUND: Encapsulation of hydrophilic drugs within liposomes can be challenging. METHODS: A novel chitosan derivative, O-palmitoyl chitosan (OPC) was synthesized from chitosan and palmitoyl chloride using methane-sulfonic acid as a solvent. The success of synthesis was confirmed by Fourier transform infra-red (FT-IR) spectroscopy and proton NMR spectroscopy (H-NMR). Liposomes encapsulating ferrous sulphate as a model hydrophilic drug for intestinal delivery were prepared with or without OPC inclusion (Lipo-Fe and OPC-Lipo-Fe). RESULTS: Entrapment of iron was significantly higher in OPC containing liposomes compared to controls. Quantitative iron absorption from the OPC liposomes was significantly higher (1.5-fold P<0.05) than free ferrous sulphate controls. Qualitative uptake analysis by confocal imaging using coumarin-6 dye loaded liposomes also indicated higher cellular uptake and internalization of the OPC-containing liposomes. CONCLUSION: These findings suggest that addition of OPC during liposome preparation creates robust vesicles that have improved mucoadhesive and absorption enhancing properties. The chitosan derivative OPC therefore provides a novel alternative for formulation of delivery vehicles targeting intestinal absorption.

Type: Article
Title: Hydrophobically-modified chitosan nanoliposomes for intestinal drug delivery
Open access status: An open access version is available from UCL Discovery
DOI: 10.2147/IJN.S166901
Publisher version: https://doi.org/10.2147/IJN.S166901
Language: English
Additional information: © 2018 Zariwala et al. This work is published and licensed by Dove Medical Press Limited. The full terms of this license are available at https://www.dovepress.com/terms.php and incorporate the Creative Commons Attribution – Non Commercial (unported, v3.0) License (http://creativecommons.org/licenses/by-nc/3.0/). By accessing the work you hereby accept the Terms. Non-commercial uses of the work are permitted without any further permission from Dove Medical Press Limited, provided the work is properly attributed. For permission for commercial use of this work, please see paragraphs 4.2 and 5 of our Terms (https://www.dovepress.com/terms.php).
Keywords: gut delivery, intestinal absorption, Caco-2, ferrous sulfate
UCL classification: UCL
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences > UCL School of Pharmacy
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences > UCL School of Pharmacy > Pharmaceutics
URI: https://discovery.ucl.ac.uk/id/eprint/10051840
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