Jadoul A, Mesens J, Caers W, de Beukelaar F, Crabbe R, Preat V
Universite Catholique de Louvain, Ecole de Pharmacie, Unite de Pharmacie Galenique, Brussels, Belgium.
PURPOSE: The aim of this paper was to assess the feasibility of electrically
enhanced transdermal delivery of alniditan, a novel 5 HT1D agonist for
the treatment of migraine. METHODS: An in vitro study was first performed
to optimize the different parameters affecting iontophoresis efficiency.
The mechanism of alniditan permeation by iontophoresis was investigated.
Finally, a phase I clinical trial was performed to assess systemic delivery
of alniditan by iontophoresis. RESULTS: i) In vitro: The optimal conditions
were found with a buffer like ethanolamine at a pH of 9.5, with Ag/AgCl
electrodes and a direct current application. Alniditan permeation was enhanced
when increasing the current density, the duration of current application
and the drug concentration. Iontophoresis slightly increased drug quantities
in stratum corneum compared to passive diffusion but it strongly increased
alniditan quantities in viable skin. ii) The objective to deliver in vivo
0.5 mg of alniditan within less than 1 h was reached but an erythema was
detected at the anode. CONCLUSIONS: This study demonstrates the feasibility
of iontophoretic delivery system for antimigraine
compounds.
Publication Types:
Clinical trial
Clinical trial, phase i
PMID: 8893273, UI: 97048437