Concentration dependency in nicotine skin penetration flux from aqueous solutions reflects vehicle induced changes in nicotine stratum corneum retention

Kuswahyuning, Rina and Roberts, Michael S. (2014) Concentration dependency in nicotine skin penetration flux from aqueous solutions reflects vehicle induced changes in nicotine stratum corneum retention. Pharmaceutical Research, 31 6: 1501-1511. doi:10.1007/s11095-013-1256-4


Author Kuswahyuning, Rina
Roberts, Michael S.
Title Concentration dependency in nicotine skin penetration flux from aqueous solutions reflects vehicle induced changes in nicotine stratum corneum retention
Journal name Pharmaceutical Research   Check publisher's open access policy
ISSN 1573-904X
0724-8741
Publication date 2014-06
Year available 2014
Sub-type Article (original research)
DOI 10.1007/s11095-013-1256-4
Open Access Status
Volume 31
Issue 6
Start page 1501
End page 1511
Total pages 11
Place of publication New York, NY, United States
Publisher Springer New York LLC
Collection year 2015
Language eng
Formatted abstract
Purpose
This study sought to understand the mechanism by which the steady state flux of nicotine across the human skin from aqueous solutions is markedly decreased at higher nicotine concentrations.

Methods
Nicotine’s steady state flux through human epidermis and its amount in the stratum corneum for a range of aqueous nicotine solutions was determined using Franz diffusion cells, with the nicotine analysed by high performance liquid chromatography (HPLC). Nicotine’s thermodynamic activity in the various solutions was estimated from its partial vapour pressure and stratum corneum hydration was determined using a corneometer. The amount of nicotine retained in the stratum corneum was estimated from the nicotine amount found in individual stratum corneum tape strips and a D-Squame determined weight for each strip.

Results
The observed steady state flux of nicotine across human epidermis was found to show a parabolic dependence on nicotine concentration, with the flux proportional to its thermodynamic activity up to a concentration of 48% w/w. The nicotine retention in the stratum corneum showed a similar dependency on concentration whereas the diffusivity of nicotine in the stratum corneum appeared to be concentration independent. This retention, in turn, could be estimated from the extent of stratum corneum hydration and the nicotine concentration in the applied solution and volume of water in the skin.

Conclusions
Nonlinear dependency of nicotine skin flux on its concentration results from a dehydration induced decrease in its stratum corneum retention at higher concentration and not dehydration induced changes nicotine diffusivity in the stratum corneum.
Keyword Nicotine thermodynamic activity
Skin penetration flux
Solute concentration
Stratum corneum hydration
Stratum corneum retention
Q-Index Code C1
Q-Index Status Confirmed Code
Institutional Status UQ

Document type: Journal Article
Sub-type: Article (original research)
Collections: Official 2015 Collection
School of Medicine Publications
 
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