An integrated pharmacokinetic and imaging evaluation of vehicle effects on solute human epidermal flux and, retention characteristics

Winckle, G., Anissimov, Y. G., Cross, S. E., Wise, G. and Roberts, M. S. (2008) An integrated pharmacokinetic and imaging evaluation of vehicle effects on solute human epidermal flux and, retention characteristics. Pharmaceutical Research, 25 1: 158-166.


Author Winckle, G.
Anissimov, Y. G.
Cross, S. E.
Wise, G.
Roberts, M. S.
Title An integrated pharmacokinetic and imaging evaluation of vehicle effects on solute human epidermal flux and, retention characteristics
Journal name Pharmaceutical Research   Check publisher's open access policy
ISSN 0724-8741
1573-904X
Publication date 2008-01
Sub-type Article (original research)
DOI 10.1007/s11095-007-9416-z
Volume 25
Issue 1
Start page 158
End page 166
Total pages 9
Editor H .L. Lee Vincent
Place of publication United States
Publisher Springer
Collection year 2009
Language eng
Subject C1
929999 Health not elsewhere classified
11 Medical and Health Sciences
Formatted abstract Objective
Our understanding of the differential effects of topically applied vehicles on solute partitioning and diffusion within the skin is presently limited. In this work, in vitro epidermal partitioning, penetration and multiphoton laser scanning microscopy (MPLSM) imaging studies were used to assess the distribution of 2-naphthol across human epidermis.

Materials and Methods

Four commonly used liquid vehicles (100% water, 20% propylene glycol (PG)/water, 50% ethanol (EtOH)/water and 100% isopropyl myristate (IPM)) were used.

Results and Discussion

The maximum flux and membrane retention of 2-naphthol from 50% EtOH/water was almost an order of magnitude or larger than from the other vehicles evaluated whereas IPM resulted in the highest membrane retention and lowest membrane penetration for 2-naphthol than other vehicles. MPLSM studies showed that 2-naphthol solute partitioned favourably into the intercellular lipids and that there was a vehicle-dependent uptake of 2-naphthol into corneocytes.

Conclusions

The integrated evaluation using in vitro penetration, epidermal retention and MPLSM imaging has shown that vehicle effects on skin penetration occurs by an alteration in the distribution of solutes between the corneocytes and intercellular lipids in addition to the well known mechanisms of altered partitioning into the stratum corneum and enhanced epidermal diffusion.

Keyword corneocyte
transdermal penetration
stratum corneum
multiphoton laser scanning microscopy
Formulations
Q-Index Code C1
Q-Index Status Confirmed Code

Document type: Journal Article
Sub-type: Article (original research)
Collections: 2009 Higher Education Research Data Collection
School of Biomedical Sciences Publications
School of Medicine Publications
 
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Created: Tue, 29 Jul 2008, 16:23:44 EST