Pharmacokinetics of Alternative Administration Routes of Melatonin: A Systematic Review

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#administration-cutaneous #administration-intranasal #administration-mucosal #administration-oral #animals

Pharmacokinetics of Alternative Administration Routes of Melatonin: A Systematic Review

Zetner et al., 2016 | Drug Res (Stuttg) | Systematic Review

Citation

Zetner D, Andersen L P H, Rosenberg J. Pharmacokinetics of Alternative Administration Routes of Melatonin: A Systematic Review. Drug Res (Stuttg). 2016-Apr;66(4):169-73. doi:10.1055/s-0035-1565083

Abstract

BACKGROUND: Melatonin is traditionally administered orally but has a poor and variable bioavailability. This study aims to present an overview of studies investigating the pharmacokinetics of alternative administration routes of melatonin. METHODS: A systematic literature search was performed and included experimental or clinical studies, investigating pharmacokinetics of alternative administration routes of melatonin in vivo. Alternative administration routes were defined as all administration routes except oral and intravenous. RESULTS: 10 studies were included in the review. Intranasal administration exhibited a quick absorption rate and high bioavailability. Transdermal administration displayed a variable absorption rate and possible deposition of melatonin in the skin. Oral transmucosal administration of melatonin exhibited a high plasma concentration compared to oral administration. Subcutaneous injection of melatonin displayed a rapid absorption rate compared to oral administration. CONCLUSION: Intranasal administration of melatonin has a large potential, and more research in humans is warranted. Transdermal application of melatonin has a possible use in a local application, due to slow absorption and deposition in the skin. Oral transmucosal administration may potentially be a clinically relevant due to avoiding first-pass metabolism. Subcutaneous injection of melatonin did not document any advantages compared to other administration routes.

Key Findings

10 studies were included in the review. Intranasal administration exhibited a quick absorption rate and high bioavailability. Transdermal administration displayed a variable absorption rate and possible deposition of melatonin in the skin. Oral transmucosal administration of melatonin exhibited a high plasma concentration compared to oral administration. Subcutaneous injection of melatonin displayed a rapid absorption rate compared to oral administration.

Outcomes Measured

  • Requires manual extraction

Population

Field Value
Population See abstract
Sample Size 10
Age Range See abstract
Condition See abstract

MeSH Terms

  • Administration, Cutaneous
  • Administration, Intranasal
  • Administration, Mucosal
  • Administration, Oral
  • Animals
  • Biological Availability
  • Humans
  • Injections, Subcutaneous
  • Melatonin

Evidence Classification

  • Level: Systematic Review
  • Publication Types: Journal Article, Systematic Review
  • Vertical: melatonin

Provenance

Source extracted via PubMed E-utilities API on 2026-04-09