Glucose-targeted niosomes deliver vasoactive intestinal peptide (VIP) to the brain

Christine Dufès, Frédéric Gaillard, I.F. Uchegbu, Andreas G. Schätzlein, Jean-Christophe Olivier, Jean-Marc Muller

Research output: Contribution to journalArticle

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Abstract

The aim of this study was to evaluate glucose-bearing niosomes as a brain targeted delivery system for the vasoactive intestinal peptide (VIP). To this end, VIP/125I-VIP-loaded glucose-bearing niosomes were intravenously injected to mice. Brain uptake was determined by measuring the radioactivity of 125I-labeled VIP using gamma-counting, after intravenous administration of VIP in solution or encapsulated in glucose-bearing niosomes or in control niosomes. VIP integrity was assessed by reversed-phase HPLC analysis of brain extracts. Distribution of 125I-VIP derived radioactivity was examined from serial brain slices. HPLC analysis confirmed the presence of intact VIP in brain after administration of VIP-loaded niosomes, but not after administration of VIP solution. Encapsulation within glucose-bearing niosomes mainly allowed a significantly higher VIP brain uptake compared to control niosomes (up to 86%, 5min after treatment). Brain distribution of intact VIP after injection of glucose-bearing niosomes, indicated that radioactivity was preferentially located in the posterior and the anterior parts of the brain, whereas it was homogeneously distributed in the whole brain after the administration of control vesicles. In conclusion, this novel vesicular formulation of VIP delivers intact VIP to particular brain regions in mice. Glucose-bearing vesicles might be therefore a novel tool to deliver drugs across the blood-brain barrier (BBB).
LanguageEnglish
Pages77-85
Number of pages9
JournalInternational Journal of Pharmaceutics
Volume285
Issue number1-2
DOIs
StatePublished - 2004

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Vasoactive Intestinal Peptide
Liposomes
Glucose
Brain
Radioactivity
High Pressure Liquid Chromatography
Blood-Brain Barrier
Intravenous Administration

Keywords

  • niosomes
  • glucose
  • vasoactive intestinal peptide
  • brain delivery
  • blood–brain barrier
  • pharmacology
  • biomedical sciences

Cite this

Dufès, C., Gaillard, F., Uchegbu, I. F., Schätzlein, A. G., Olivier, J-C., & Muller, J-M. (2004). Glucose-targeted niosomes deliver vasoactive intestinal peptide (VIP) to the brain. International Journal of Pharmaceutics, 285(1-2), 77-85. DOI: 10.1016/j.ijpharm.2004.07.020
Dufès, Christine ; Gaillard, Frédéric ; Uchegbu, I.F. ; Schätzlein, Andreas G. ; Olivier, Jean-Christophe ; Muller, Jean-Marc. / Glucose-targeted niosomes deliver vasoactive intestinal peptide (VIP) to the brain. In: International Journal of Pharmaceutics. 2004 ; Vol. 285, No. 1-2. pp. 77-85
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Dufès, C, Gaillard, F, Uchegbu, IF, Schätzlein, AG, Olivier, J-C & Muller, J-M 2004, 'Glucose-targeted niosomes deliver vasoactive intestinal peptide (VIP) to the brain' International Journal of Pharmaceutics, vol. 285, no. 1-2, pp. 77-85. DOI: 10.1016/j.ijpharm.2004.07.020

Glucose-targeted niosomes deliver vasoactive intestinal peptide (VIP) to the brain. / Dufès, Christine; Gaillard, Frédéric; Uchegbu, I.F.; Schätzlein, Andreas G.; Olivier, Jean-Christophe; Muller, Jean-Marc.

In: International Journal of Pharmaceutics, Vol. 285, No. 1-2, 2004, p. 77-85.

Research output: Contribution to journalArticle

TY - JOUR

T1 - Glucose-targeted niosomes deliver vasoactive intestinal peptide (VIP) to the brain

AU - Dufès,Christine

AU - Gaillard,Frédéric

AU - Uchegbu,I.F.

AU - Schätzlein,Andreas G.

AU - Olivier,Jean-Christophe

AU - Muller,Jean-Marc

PY - 2004

Y1 - 2004

N2 - The aim of this study was to evaluate glucose-bearing niosomes as a brain targeted delivery system for the vasoactive intestinal peptide (VIP). To this end, VIP/125I-VIP-loaded glucose-bearing niosomes were intravenously injected to mice. Brain uptake was determined by measuring the radioactivity of 125I-labeled VIP using gamma-counting, after intravenous administration of VIP in solution or encapsulated in glucose-bearing niosomes or in control niosomes. VIP integrity was assessed by reversed-phase HPLC analysis of brain extracts. Distribution of 125I-VIP derived radioactivity was examined from serial brain slices. HPLC analysis confirmed the presence of intact VIP in brain after administration of VIP-loaded niosomes, but not after administration of VIP solution. Encapsulation within glucose-bearing niosomes mainly allowed a significantly higher VIP brain uptake compared to control niosomes (up to 86%, 5min after treatment). Brain distribution of intact VIP after injection of glucose-bearing niosomes, indicated that radioactivity was preferentially located in the posterior and the anterior parts of the brain, whereas it was homogeneously distributed in the whole brain after the administration of control vesicles. In conclusion, this novel vesicular formulation of VIP delivers intact VIP to particular brain regions in mice. Glucose-bearing vesicles might be therefore a novel tool to deliver drugs across the blood-brain barrier (BBB).

AB - The aim of this study was to evaluate glucose-bearing niosomes as a brain targeted delivery system for the vasoactive intestinal peptide (VIP). To this end, VIP/125I-VIP-loaded glucose-bearing niosomes were intravenously injected to mice. Brain uptake was determined by measuring the radioactivity of 125I-labeled VIP using gamma-counting, after intravenous administration of VIP in solution or encapsulated in glucose-bearing niosomes or in control niosomes. VIP integrity was assessed by reversed-phase HPLC analysis of brain extracts. Distribution of 125I-VIP derived radioactivity was examined from serial brain slices. HPLC analysis confirmed the presence of intact VIP in brain after administration of VIP-loaded niosomes, but not after administration of VIP solution. Encapsulation within glucose-bearing niosomes mainly allowed a significantly higher VIP brain uptake compared to control niosomes (up to 86%, 5min after treatment). Brain distribution of intact VIP after injection of glucose-bearing niosomes, indicated that radioactivity was preferentially located in the posterior and the anterior parts of the brain, whereas it was homogeneously distributed in the whole brain after the administration of control vesicles. In conclusion, this novel vesicular formulation of VIP delivers intact VIP to particular brain regions in mice. Glucose-bearing vesicles might be therefore a novel tool to deliver drugs across the blood-brain barrier (BBB).

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KW - glucose

KW - vasoactive intestinal peptide

KW - brain delivery

KW - blood–brain barrier

KW - pharmacology

KW - biomedical sciences

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DO - 10.1016/j.ijpharm.2004.07.020

M3 - Article

VL - 285

SP - 77

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JO - International Journal of Pharmaceutics

T2 - International Journal of Pharmaceutics

JF - International Journal of Pharmaceutics

SN - 0378-5173

IS - 1-2

ER -

Dufès C, Gaillard F, Uchegbu IF, Schätzlein AG, Olivier J-C, Muller J-M. Glucose-targeted niosomes deliver vasoactive intestinal peptide (VIP) to the brain. International Journal of Pharmaceutics. 2004;285(1-2):77-85. Available from, DOI: 10.1016/j.ijpharm.2004.07.020