Transdermal penetration of vasoconstrictors - Present understanding and assessment of the human epidermal flux and retention of free bases and ion-pairs

Cross, SE, Thompson, MJ and Roberts, MS (2003) Transdermal penetration of vasoconstrictors - Present understanding and assessment of the human epidermal flux and retention of free bases and ion-pairs. Pharmaceutical Research, 20 2: 270-274. doi:10.1023/A:1022235507186


Author Cross, SE
Thompson, MJ
Roberts, MS
Title Transdermal penetration of vasoconstrictors - Present understanding and assessment of the human epidermal flux and retention of free bases and ion-pairs
Journal name Pharmaceutical Research   Check publisher's open access policy
ISSN 0724-8741
Publication date 2003-01-01
Year available 2003
Sub-type Article (original research)
DOI 10.1023/A:1022235507186
Open Access Status Not yet assessed
Volume 20
Issue 2
Start page 270
End page 274
Total pages 5
Editor Vincent H L Lee
Place of publication USA
Publisher Kluwer Academic / Plenum Publishers
Language eng
Subject C1
320501 Pharmaceutical Sciences and Pharmacy
730199 Clinical health not specific to particular organs, diseases and conditions
Abstract Purpose. As reductions in dermal clearance increase the residence time of solutes in the skin and underlying tissues we compared the topical penetration of potentially useful vasoconstrictors (VCs) through human epidermis as both free bases and ion-pairs with salicylic acid (SA). Methods. We determined the in vitro epidermal flux of ephedrine, naphazoline, oxymetazoline, phenylephrine, and xylometazoline applied as saturated solutions in propylene glycol: water (1: 1) and of ephedrine, naphazoline and tetrahydrozoline as 10% solutions of 1: 1 molar ratio ion-pairs with SA in liquid paraffin. Results. As free bases, ephedrine had the highest maximal flux, Jmax = 77.4 +/- 11.7 mug/cm(2)/h, being 4-fold higher than tetrahydrozoline and xylometazoline, 6-fold higher than phenylephrine, 10-fold higher than naphazoline and 100-fold higher than oxymetazoline. Stepwise regression of solute physicochemical properties identified melting point as the most significant predictor of flux. As ion-pairs with SA, ephedrine and naphazoline had similar fluxes (11.5 +/- 2.3 and 12.0 +/- 1.6 mug/cm(2)/h respectively), whereas tetrahydrozoline was approximately 3-fold slower. Corresponding fluxes of SA from the ion-pairs were 18.6 +/- 0.6, 7.8 +/- 0.8 and 1.1 +/- 0.1 respectively. Transdermal transport of VC's is discussed. Conclusions. Epidermal retention of VCs and SA did not correspond to their molar ratio on application and confirmed that following partitioning into the stratum corneum, ion-pairs separate and further penetration is governed by individual solute characteristics.
Keyword Chemistry, Multidisciplinary
Pharmacology & Pharmacy
Vasoconstrictor
Transdermal
Percutaneous Absorption
Epidermal Retention
Physicochemical Properties
Topical Decongestant
Vasoactive Drugs
Salicylic-acid
Skin
Iontophoresis
Absorption
Transport
Q-Index Code C1
Institutional Status UQ

Document type: Journal Article
Sub-type: Article (original research)
Collections: Excellence in Research Australia (ERA) - Collection
2004 Higher Education Research Data Collection
School of Medicine Publications
 
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Citation counts: TR Web of Science Citation Count  Cited 4 times in Thomson Reuters Web of Science Article | Citations
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Created: Wed, 15 Aug 2007, 11:39:43 EST