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Percutaneous absorption of steroids: Relative contributions of epidermal penetration and dermal clearance

  • O. Siddiqui
  • M. S. Roberts
  • A. E. Polack
Article

Abstract

The permeation of triamcinolone, hydrocortisone, prednisolone, corticosterone, triamdnolone acetonide, testosterone, and betamethasone-17-valerate through excised human stratum corneum was quantified. The time course of permeation could be adequately described by a simple diffusion model suggesting that shunt transport may not be important. The disappearance of these steroids from aqueous solutions applied to human and rat dermis was also monitored. The concentrations of unbound steroid in the viable epidermis appeared to be mainly related to the blood perfusion rate in the dermis and, more importantly, to the lipophilicity of the steroid. The most lipophilic steroids penetrated the human epidermis at the fastest rates but are cleared from the viable epidermis at rates comparable to those found for more polar steroids.

Key words

steroids epidermal penetration dermal clearance shunt transport dermal transport 

Glossary

Symbols

A

Intercept for fraction remaining (or area)

B

Intercept for fraction remaining (= 1−A)

Cv

Concentration in vehicle

Css

Steady state concentration

Cl

Clearance

D

Diffusion coefficient

h

Thickness

Jss

Steady state flux (=kpCv)

K

Partition coefficient between stratum corneum and vehicle

k

Pseudo-first-order rate constant for dermal disappearance

kp

Permeability coefficient (=KD/h)

M

Cumulative amount

MRT

Mean residence time

n

Integer value

t

Time

tL

Lag time

R

Partition coefficient between dermis and the aqueous solution

r0

Rate of input

V1

Donor volume

V2

Volume of distribution in dermis

Vdss

Volume of distribution at steady state

%CV

Percentage coefficient of variation (SD×100/mean)

Subscripts

d

Dermis

e

Epidermis (intracellular/intercellular)

s

Shunts

total

Sum of epidermal and dermal contributions

λ1

Fast rate constant for dermal disappearance

λ2

Slow rate constant for dermal disappearance

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Copyright information

© Plenum Publishing Corporation 1989

Authors and Affiliations

  • O. Siddiqui
    • 1
  • M. S. Roberts
    • 1
  • A. E. Polack
    • 1
  1. 1.School of PharmacyUniversity of TasmaniaHobartAustralia

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