Transdermal delivery of methotrexate for pediatrics using silicon microneedles

Ther Deliv. 2013 May;4(5):543-51. doi: 10.4155/tde.13.24.

Abstract

Background: The objective of this work was to study transdermal delivery of methotrexate using silicon microneedles and simulate plasma concentrations using a population pharmacokinetic model.

Results: Characterization of silicon microneedles was carried out by scanning electron microscopy, transepidermal water loss, methylene blue staining, calcein imaging, pore permeability index and confocal microscopy, which confirmed the formation of microchannels. In vitro permeation studies were performed to study the enhancement in transdermal delivery following microporation.

Conclusion: Simulation data demonstrated that with 16, 64, 128 and 192 microneedles, mean plasma concentrations of 0.3, 1.4, 2.8 and 4.2 ng/ml, respectively, can be achieved. Thus, therapeutically relevant doses could be delivered in pediatrics by increasing the number of microneedles and patch area.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Administration, Cutaneous
  • Animals
  • Antimetabolites, Antineoplastic / administration & dosage*
  • Antimetabolites, Antineoplastic / pharmacokinetics
  • Child
  • Drug Delivery Systems*
  • Humans
  • Male
  • Methotrexate / administration & dosage*
  • Methotrexate / pharmacokinetics
  • Microinjections
  • Microscopy, Confocal
  • Microscopy, Electron, Scanning
  • Models, Biological
  • Needles
  • Rats
  • Rats, Hairless
  • Silicon / chemistry
  • Skin Absorption*
  • Staining and Labeling
  • Transdermal Patch
  • Water Loss, Insensible

Substances

  • Antimetabolites, Antineoplastic
  • Methotrexate
  • Silicon