UNIGE document Scientific Article
previous document  unige:22643  next document
add to browser collection

Effect of amino acid sequence on transdermal iontophoretic peptide delivery

Published in European Journal of Pharmaceutical Sciences. 2005, vol. 26, no. 5, p. 429-37
Abstract The objective of this study was to investigate the effect of amino acid sequence on the transdermal delivery of peptides by iontophoresis. Structurally related, cationic tripeptides based on the residues at positions (i) 6-8 in LHRH (Ac-X-Leu-Arg-NH(2)) and (ii) 3-5 in octreotide (Ac-X-dTrp-Lys-NH(2)) were studied. Iontophoretic transport experiments were conducted using porcine skin in vitro to investigate the dependence of flux on peptide concentration. Co-iontophoresis of acetaminophen enabled deconvolution of the contributions of electromigration (EM) and electroosmosis (EO) and the calculation of an electroosmotic inhibition factor (IF). A two-fold increase in donor peptide concentration increased iontophoretic flux for most peptides, and electroosmotic inhibition for dNal-containing tripeptides. The improvement in transport and the impact on the EM and EO components were peptide-specific. A reduction in the number of competing ions in the formulation significantly increased transport and, specifically, the EM contribution; it also increased IF of compounds with a propensity to interact with the membrane. No monotonic dependence of flux on either molecular weight or lipophilicity was observed. Iontophoretic peptide transport could not be rationalized in terms of either peptide molecular weight or computational 2D estimates of lipophilicity. Data suggest that a more complex three-dimensional approach is required to develop structure permeation relationships governing iontophoretic peptide delivery.
Keywords AdministrationCutaneousAmino Acid SequenceAnimalsIontophoresisPeptides/administration & dosageSkin/metabolismSwine
PMID: 16143501
Full text
Article (Published version) (342 Kb) - document accessible for UNIGE members only Limited access to UNIGE
(ISO format)
SCHUETZ, Yannic et al. Effect of amino acid sequence on transdermal iontophoretic peptide delivery. In: European Journal of Pharmaceutical Sciences, 2005, vol. 26, n° 5, p. 429-37. https://archive-ouverte.unige.ch/unige:22643

182 hits

0 download


Deposited on : 2012-08-29

Export document
Format :
Citation style :