Skin electroporation: rapid measurements of the transdermal voltage and flux of four fluorescent molecules show a transition to large fluxes near 50 V

J Pharm Sci. 1998 Nov;87(11):1368-74. doi: 10.1021/js980071k.

Abstract

Large molecular fluxes and tight control are highly desired for transdermal drug delivery, which motivated this study of molecular transport due to high voltage pulsing. We used a flow-through sampling system (time resolution of approximately 14 s) to measure the response of human skin in vitro to a series of exponential pulses (time constant of 1 ms; peak transdermal voltages [Uskin,0] of 0 V to approximately 300 V, one pulse every 5.6 s). Four negatively charged, hydrophilic fluorescent tracer molecules were employed: sulforhodamine, lucifer yellow, cascade blue, and calcein (molecular weights of 450 to 625 Da). Although differences in their molecular transport profiles were observed, all four molecules exhibited a transition from small to large fluxes at Uskin,0 approximately 50 V. This behavior may reflect a transition from electroporation of the skin's appendages to electroporation of the multilamellar bilayer membranes within the stratum corneum.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Electroporation*
  • Fluoresceins / metabolism
  • Fluorescent Dyes / metabolism*
  • Humans
  • Isoquinolines / metabolism
  • Organometallic Compounds / metabolism
  • Organophosphorus Compounds / metabolism
  • Skin / metabolism
  • Skin Absorption
  • Skin Physiological Phenomena*

Substances

  • Fluoresceins
  • Fluorescent Dyes
  • Isoquinolines
  • Organometallic Compounds
  • Organophosphorus Compounds
  • Cascade Blue
  • lucifer yellow
  • fluorexon