Transdermal iontophoretic delivery of triptorelin in vitro

J Pharm Sci. 2005 Oct;94(10):2175-82. doi: 10.1002/jps.20433.

Abstract

The feasibility of delivering triptorelin ([D-Trp6]LHRH) by transdermal iontophoresis was evaluated in vitro. Peptide electrotransport at different current densities and donor concentrations was measured across porcine ear skin. The concomitant delivery of an electroosmotic marker enabled calculation of the respective contributions of electromigration (EM) and electroosmosis (EO) to iontophoretic delivery. At a given concentration (3 mM), a threefold increase in current density produced a corresponding increase in the cumulative amount of peptide present in the receptor compartment. Conversely, doubling the concentration to 6 mM produced a twofold reduction in the amount of peptide delivered, partly due to a concentration-dependent inhibition of EO. EM was revealed to be the predominant transport mechanism, accounting for 80% of overall delivery. Finally, despite the inhibition of EO, the results indicate that application of an iontophoretic current of 0.8 mA over a relatively small contact area (4 cm2) would provide a delivery rate of 36 microg/h, largely sufficient for therapeutic requirements.

Publication types

  • Comparative Study

MeSH terms

  • Acetaminophen / metabolism
  • Administration, Cutaneous
  • Animals
  • Chemistry, Pharmaceutical
  • Drug Stability
  • Ear
  • In Vitro Techniques
  • Iontophoresis*
  • Luteolytic Agents / metabolism*
  • Osmosis
  • Peptide Fragments / chemistry
  • Peptide Fragments / metabolism
  • Permeability
  • Skin / chemistry
  • Skin / metabolism*
  • Skin Absorption*
  • Swine
  • Time Factors
  • Triptorelin Pamoate / chemistry
  • Triptorelin Pamoate / metabolism*

Substances

  • Luteolytic Agents
  • Peptide Fragments
  • Triptorelin Pamoate
  • Acetaminophen