Hydrophobically-modified chitosan nanoliposomes for intestinal drug delivery

Mohammed Gulrez Zariwala, Harshada Bendre, Anatoliy Markiv, Sebastien Farnaud, Derek Renshaw, Kevin M G Taylor, Satyanarayana Somavarapu

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Abstract

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). 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. 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.
Original languageEnglish
Pages (from-to)5837-5848
Number of pages12
JournalInternational Journal of Nanomedicine
Volume13
DOIs
Publication statusPublished - 27 Sep 2018

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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. 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.

Keywords

  • Liposomes
  • Ferrous sulphate
  • Caco-2
  • Gut delivery
  • Intestinal absorption

ASJC Scopus subject areas

  • Pharmacology, Toxicology and Pharmaceutics(all)

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