Effect of Microneedle Type on Transdermal Permeation of Rizatriptan

AAPS PharmSciTech. 2017 Jul;18(5):1495-1506. doi: 10.1208/s12249-016-0702-0. Epub 2017 Jan 11.

Abstract

The present study was aimed to investigate the effect of salient microneedle (MN) geometry parameters like length, density, shape and type on transdermal permeation of rizatriptan (RIZ). Studies were carried out using two types of MN devices viz. AdminPatch® arrays (ADM) (0.6, 0.9, 1.2 and 1.5 mm lengths) and laboratory-fabricated polymeric MNs (PMs) of 0.6 mm length. In the case of the PMs, arrays were applied three times at different places within a 1.77-cm2 skin area (PM-3) to maintain the MN density closer to 0.6 mm ADM. Histological studies revealed that PM, owing to their geometry/design, formed wider and deeper microconduits when compared to ADM of similar length. Approximately 4.9- and 4.2-fold increases in the RIZ steady-state flux values were observed with 1.5 mm ADM and PM-3 applications when compared to the passive studies. A good correlation between different dimensionless parameters like the amount of RIZ permeated (C t /C s), thickness (h/L) and surface area (S a/L 2) of the skin was observed with scaling analyses. Numerical simulations provided further information regarding the distribution of RIZ in MN-treated skin after application of different MNs. Overall, the study suggests that MN application enhances the RIZ transdermal permeation and the geometrical parameters of MNs play an important role in the degree enhancement.

Keywords: histological sections; microneedle geometry; microneedles; numerical simulations; rizatriptan; scaling analyses; transdermal enhancement.

MeSH terms

  • Administration, Cutaneous
  • Drug Delivery Systems / instrumentation
  • Needles / standards*
  • Numerical Analysis, Computer-Assisted
  • Serotonin Receptor Agonists / chemistry
  • Serotonin Receptor Agonists / pharmacokinetics
  • Skin / pathology
  • Skin Absorption
  • Triazoles* / chemistry
  • Triazoles* / pharmacokinetics
  • Tryptamines* / chemistry
  • Tryptamines* / pharmacokinetics

Substances

  • Serotonin Receptor Agonists
  • Triazoles
  • Tryptamines
  • rizatriptan