Pharmaceutical Research

, Volume 33, Issue 7, pp 1564–1575 | Cite as

Skin Absorption of Anions: Part One. Methodology for In Vitro Cutaneous Absorption Measurements

  • Raphaël Paweloszek
  • Stéphanie Briançon
  • Yves Chevalier
  • Nicole Gilon-Delepine
  • Jocelyne Pelletier
  • Marie-Alexandrine Bolzinger
Research Paper

Abstract

Purpose

Measurement of skin absorption of ions requires specific experimental protocols regarding the use of pig skin as a model, the viability of excised skin in water medium over 24 h, the presence of endogenous ions, and evaluation of the contributions of facilitated transport through ion channels and ion transporters.

Method

Absorption experiments of halide anions F, Cl, Br and I in excised skin were performed in Franz diffusion cells. Experiments were performed on human and porcine skin under various conditions so as to define and validate experimental protocols.

Results

The distributions of endogenous ions and the absorption kinetics of halide ions were similar in both porcine and human skin models. Fresh skin kept its viability over 24 h in salt-free water, allowing experiments following OECD guidelines. Permeation increased in the order F < Cl < Br < I for all receptor media and skin samples. Absorption was larger in fresh skin due to the transport through chloride channels or exchangers.

Conclusion

Skin absorption experiments of ions in Franz cells rely on working with fresh excised skin (human or porcine) and pure water as receptor fluid. Experiments with chloride blockers or frozen/thawed skin allow discriminating passive diffusion and facilitated transport.

KEYWORDS

anion halide ion permeation skin absorption 

ABBREVIATIONS

CaCC

Ca2+ activated Cl channels

CFTR

Cystic fibrosis transmembrane conductance regulator

ClC

Chloride channel

D

Dermis

DF

Donor fluid

DIDS

4,4′-Diisothiocyanatostilbene-2,2′-disulfonic acid

HBSS

Hank’s balanced salt solution. It contains 1 g.L−1 of glucose in its composition.

IAA-94

Indanyloxyacetic acid

IC

Ion chromatography

ICP-OES

Inductively coupled plasma optical emission spectrometry

LDH

Lactate deshydrogenase

NCC

Sodium-chloride symporter (also known as Na+-Cl co-transporter)

NIS

Sodium-iodide symporter

NKCC

Sodium-potassium-chloride co-transporter

RF

Receptor fluid

SC

Stratum corneum

SSG

Serum saline (physiological serum saline solution NaCl 9 g.L−1) containing 1 g.L−1 of glucose

VE

Viable epidermis

WG

Ultrapure water (resistivity >18 MΩ.cm at 25°C) containing 1 g.L−1 of glucose

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Copyright information

© Springer Science+Business Media New York 2016

Authors and Affiliations

  • Raphaël Paweloszek
    • 1
  • Stéphanie Briançon
    • 1
  • Yves Chevalier
    • 1
  • Nicole Gilon-Delepine
    • 2
  • Jocelyne Pelletier
    • 1
  • Marie-Alexandrine Bolzinger
    • 1
  1. 1.Univ Lyon, Université Lyon 1, CNRS, UMR5007, LAGEP - Laboratoire de Dermopharmacie et Cosmétologie Faculté de Pharmacie de LyonVilleurbanneFrance
  2. 2.Univ Lyon, Université Lyon 1, CNRS, UMR5280, Institut des Sciences Analytiques (ISA)VilleurbanneFrance

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