Preliminary evaluation of transdermal delivery of melatonin in human subjects

B. J. Lee, K. A. Parrott, J. W. Ayres, Robert Sack

Research output: Contribution to journalArticle

57 Citations (Scopus)

Abstract

A transdermal delivery device (TDD)1 was applied to four human subjects to investigate whether melatonin (MT) could penetrate through human skin. The TDD (total surface area of 3.80 cm2) was applied to the forearm of each subject. Plasma MT concentrations increased above baseline in approximately 2-4 hours, although steady state was not achieved in the 8-hour study period. Intersubject variation of plasma MT among four subjects was noted. Urinary excretion of 6-sulphatoxymelatonin (6-STMT), a major metabolite of MT in humans, increased as plasma MT concentrations increased. Cumulative amounts of urinary 6-STMT increased over a 6-hour period when the TDD was applied and were three times greater than in controls. The urinary excretion rate of 6- STMT was statistically correlated with plasma MT concentration among subjects (r2 = 0.77). These data suggest that the urinary excretion rate of 6-STMT can be used as an index of MT plasma concentrations in human subjects. Although an intersubject variability in both plasma MT concentration and urinary excretion rate of 6-STMT was noted, it was evident that MT can be delivered transdermally in human subjects.

Original languageEnglish (US)
Pages (from-to)337-346
Number of pages10
JournalResearch Communications in Molecular Pathology and Pharmacology
Volume85
Issue number3
StatePublished - 1994

Fingerprint

Melatonin
Plasmas
Equipment and Supplies
Metabolites
Forearm
Skin
6-sulfatoxymelatonin

ASJC Scopus subject areas

  • Pathology and Forensic Medicine
  • Pharmacology, Toxicology and Pharmaceutics(all)

Cite this

Preliminary evaluation of transdermal delivery of melatonin in human subjects. / Lee, B. J.; Parrott, K. A.; Ayres, J. W.; Sack, Robert.

In: Research Communications in Molecular Pathology and Pharmacology, Vol. 85, No. 3, 1994, p. 337-346.

Research output: Contribution to journalArticle

Lee, B. J. ; Parrott, K. A. ; Ayres, J. W. ; Sack, Robert. / Preliminary evaluation of transdermal delivery of melatonin in human subjects. In: Research Communications in Molecular Pathology and Pharmacology. 1994 ; Vol. 85, No. 3. pp. 337-346.
@article{afe8ae5166104280a7400cbe8c85a93c,
title = "Preliminary evaluation of transdermal delivery of melatonin in human subjects",
abstract = "A transdermal delivery device (TDD)1 was applied to four human subjects to investigate whether melatonin (MT) could penetrate through human skin. The TDD (total surface area of 3.80 cm2) was applied to the forearm of each subject. Plasma MT concentrations increased above baseline in approximately 2-4 hours, although steady state was not achieved in the 8-hour study period. Intersubject variation of plasma MT among four subjects was noted. Urinary excretion of 6-sulphatoxymelatonin (6-STMT), a major metabolite of MT in humans, increased as plasma MT concentrations increased. Cumulative amounts of urinary 6-STMT increased over a 6-hour period when the TDD was applied and were three times greater than in controls. The urinary excretion rate of 6- STMT was statistically correlated with plasma MT concentration among subjects (r2 = 0.77). These data suggest that the urinary excretion rate of 6-STMT can be used as an index of MT plasma concentrations in human subjects. Although an intersubject variability in both plasma MT concentration and urinary excretion rate of 6-STMT was noted, it was evident that MT can be delivered transdermally in human subjects.",
author = "Lee, {B. J.} and Parrott, {K. A.} and Ayres, {J. W.} and Robert Sack",
year = "1994",
language = "English (US)",
volume = "85",
pages = "337--346",
journal = "Research Communications in Molecular Pathology and Pharmacology",
issn = "0034-5164",
publisher = "PJD Publications Ltd",
number = "3",

}

TY - JOUR

T1 - Preliminary evaluation of transdermal delivery of melatonin in human subjects

AU - Lee, B. J.

AU - Parrott, K. A.

AU - Ayres, J. W.

AU - Sack, Robert

PY - 1994

Y1 - 1994

N2 - A transdermal delivery device (TDD)1 was applied to four human subjects to investigate whether melatonin (MT) could penetrate through human skin. The TDD (total surface area of 3.80 cm2) was applied to the forearm of each subject. Plasma MT concentrations increased above baseline in approximately 2-4 hours, although steady state was not achieved in the 8-hour study period. Intersubject variation of plasma MT among four subjects was noted. Urinary excretion of 6-sulphatoxymelatonin (6-STMT), a major metabolite of MT in humans, increased as plasma MT concentrations increased. Cumulative amounts of urinary 6-STMT increased over a 6-hour period when the TDD was applied and were three times greater than in controls. The urinary excretion rate of 6- STMT was statistically correlated with plasma MT concentration among subjects (r2 = 0.77). These data suggest that the urinary excretion rate of 6-STMT can be used as an index of MT plasma concentrations in human subjects. Although an intersubject variability in both plasma MT concentration and urinary excretion rate of 6-STMT was noted, it was evident that MT can be delivered transdermally in human subjects.

AB - A transdermal delivery device (TDD)1 was applied to four human subjects to investigate whether melatonin (MT) could penetrate through human skin. The TDD (total surface area of 3.80 cm2) was applied to the forearm of each subject. Plasma MT concentrations increased above baseline in approximately 2-4 hours, although steady state was not achieved in the 8-hour study period. Intersubject variation of plasma MT among four subjects was noted. Urinary excretion of 6-sulphatoxymelatonin (6-STMT), a major metabolite of MT in humans, increased as plasma MT concentrations increased. Cumulative amounts of urinary 6-STMT increased over a 6-hour period when the TDD was applied and were three times greater than in controls. The urinary excretion rate of 6- STMT was statistically correlated with plasma MT concentration among subjects (r2 = 0.77). These data suggest that the urinary excretion rate of 6-STMT can be used as an index of MT plasma concentrations in human subjects. Although an intersubject variability in both plasma MT concentration and urinary excretion rate of 6-STMT was noted, it was evident that MT can be delivered transdermally in human subjects.

UR - http://www.scopus.com/inward/record.url?scp=0027992506&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=0027992506&partnerID=8YFLogxK

M3 - Article

C2 - 7827808

AN - SCOPUS:0027992506

VL - 85

SP - 337

EP - 346

JO - Research Communications in Molecular Pathology and Pharmacology

JF - Research Communications in Molecular Pathology and Pharmacology

SN - 0034-5164

IS - 3

ER -