Title
Percutaneous absorption of mexoryl SX® in human volunteers: Comparison with in vitro data
Author
Benech-Kieffer, F.
Meuling, W.J.A.
Leclerc, C.
Roza, L.
Leclaire, J.
Nohynek, G.
TNO Voeding
Publication year
2003
Abstract
The potential human health risk of UV filters depends on their toxicity and the human systemic exposure which is a function of the extent of percutaneous absorption of the topically applied substance into the human organism. Using a 'mass balance' approach, a study was designed to investigate the systemically absorbed dose of [14C]-Mexoryl SX® in humans after topical application of a typical sunscreen emulsion. In addition, to assess the correlation with in vitro experiments, the percutaneous absorption of this UVA filter through isolated human skin was measured under identical exposure conditions. When applied in vivo for a period of 4 h, 89-94% of the applied radioactivity was recovered from the wash-off samples. In urine samples, the radioactivity slightly exceeded background levels and corresponded maximally to 0.014% of the topically applied dose. No radioactivity was measured in blood or faeces sampled up to 120 h after application. In vitro, 24 h after a 4-hour application, [14C]-Mexoryl SX remained primarily on the skin surface. The mean in vitro absorption over 24 h, adding up the amounts found in the dermis and receptor fluid, was 0.16% of the applied dose. It is concluded from the in vivo pharmacokinetic results that the systemically absorbed dose of [14C]-Mexoryl SX is less than 0.1%. The order of magnitude of this value correlates well with the corresponding in vitro data which overestimate the in vivo results as previously observed with other hydrophilic compounds. This study demonstrates that, under realistic exposure conditions, the human systemic exposure to this UVA filter is negligible and poses no risk to human health. Copyright © 2003 S. Karger AG, Basel.
Subject
Nutrition Health
Physiological Sciences
Human skin
Mass balance
Mexoryl SX®
Percutaneous absorption
Sunscreen
carbon 14
mexoryl sr
sulfonic acid derivative
sunscreen
terephthalylidene dicamphor sulfonic acid
unclassified drug
adult
article
blood sampling
correlation analysis
dermis
drug absorption
drug exposure
feces analysis
human
human experiment
human tissue
in vitro study
male
normal human
priority journal
radioactivity
single drug dose
skin absorption
skin surface
urinalysis
Administration, Topical
Adult
Bornanes
Camphor
Diffusion
Diffusion Chambers, Culture
Half-Life
Humans
Male
Mesylates
Skin Absorption
Sulfonic Acids
Sunscreening Agents
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http://resolver.tudelft.nl/uuid:6ca992b7-ef4f-493a-b20f-174cb70e7578
DOI
https://doi.org/10.1159/000072929
TNO identifier
237332
ISSN
1422-2868
Source
Skin Pharmacology and Applied Skin Physiology, 16 (6), 343-355
Document type
article