Release of Benzimidazole and Benzylidene Camphor from Topical Sunscreen Formulations

Aghazarian, V.; Tchiakpe, L.; Reynier, Jean-Pierre; Gayte-Sorbier, A

doi:10.1081/ddc-100102299

Cited by 19 publications

(10 citation statements)

References 7 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…With 5% 4-MBC, the increase (159% of control) corresponded to the increase (154% of control) produced by an oral dose of 337 mg/kg/day, which is close to the oral ED 50 . 4-MBC exhibits significant penetration through skin of hairless rats from a 6% solution in either a W/O emulsion or oily gels (8). BP-3 is also dermally absorbed in rats (35).…”

Section: Discussionmentioning

confidence: 99%

“…Evidence for absorption by human skin has been presented for 4-MBC, Bp-3, and OD-PABA (6,7,9,10); 4-MBC also penetrates a folioxane membrane, a model for human skin (8). Skin penetration may vary between compounds, as indicated by lower penetration of OMC as compared to Bp-3 (9,36), and appears to be influenced by the formulation (8,36). Such kinetic differences may be of importance from a toxicologic point of view, but present knowledge is too incomplete to provide a picture of the general human exposure to UV screens.…”

Section: Discussionmentioning

confidence: 99%

“…The average amount of oil retained after 15 sec immersion was 1.35 ± 0.13 g, and the additional amount applied by the brush was 1.4 ± 0.08 g. Thus, the total amount of oil was 2.75 g/treatment or 5.5 g/day, yielding total amounts of 4-MBC applied to the skin per day of 137.5, 275, and 412.5 mg for 2.5, 5.0, and 7.5% 4-MBC concentrations, respectively. According to in vitro data (8), the penetration of 4-MBC through hairless rat skin is 0.6% from oily gels or 0.4% from a water in oil (W/O) emulsion. Assuming 0.6% penetration, the dose absorbed from a 5% 4-MBC solution in oil can be tentatively calculated as 37 mg/kg/day based on mean body weight of the 5% group.…”

Section: In Vivo Studiesmentioning

confidence: 99%

“…Humans can be exposed to UV screens by dermal absorption (6)(7)(8)(9) or through the food chain. The UV screen benzophenone-3 (Bp-3) and its metabolite 2,4-dihydroxybenzophenone have been detected in human urine from 4 hr after application of commercially available sunscreen products to the skin (7,10).…”

mentioning

confidence: 99%

See 3 more Smart Citations

In vitro and in vivo estrogenicity of UV screens.

Schlumpf

Cotton

Conscience

et al. 2001

Environ Health Perspect

718

287

View full text Add to dashboard Cite

Ultraviolet (UV) screens are increasingly used as a result of growing concern about UV radiation and skin cancer; they are also added to cosmetics and other products for light stability. Recent data on bioaccumulation in wildlife and humans point to a need for in-depth analyses of systemic toxicology, in particular with respect to reproduction and ontogeny. We examined six frequently used UVA and UVB screens for estrogenicity in vitro and in vivo. In MCF-7 breast cancer cells, five out of six chemicals, that is, benzophenone-3 (Bp-3), homosalate (HMS), 4-methyl-benzylidene camphor (4-MBC), octyl-methoxycinnamate (OMC), and octyl-dimethyl-PABA (OD-PABA), increased cell proliferation with median effective concentrations (EC(50)) values between 1.56 and 3.73 microM, whereas butyl-methoxydibenzoylmethane (B-MDM) was inactive. Further evidence for estrogenic activity was the induction of pS2 protein in MCF-7 cells and the blockade of the proliferative effect of 4-MBC by the estrogen antagonist ICI 182,780. In the uterotrophic assay using immature Long-Evans rats that received the chemicals for 4 days in powdered feed, uterine weight was dose-dependently increased by 4-MBC (ED(50 )309mg/kg/day), OMC (ED(50) 935 mg/kg/day), and weakly by Bp-3 (active at 1,525 mg/kg/day). Three compounds were inactive by the oral route in the doses tested. Dermal application of 4-MBC to immature hairless (hr/hr) rats also increased uterine weight at concentrations of 5 and 7.5% in olive oil. Our findings indicate that UV screens should be tested for endocrine activity, in view of possible long-term effects in humans and wildlife.

show abstract

Section: Discussionmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

Section: In Vivo Studiesmentioning

confidence: 99%

mentioning

confidence: 99%

See 2 more Smart Citations

In vitro and in vivo estrogenicity of UV screens.

Schlumpf

Cotton

Conscience

et al. 2001

Environ Health Perspect

718

287

View full text Add to dashboard Cite

show abstract

“…BP-3 is also dermally absorbed in rats (35). Evidence for absorption by human skin has been presented for 4-MBC, Bp-3, and OD-PABA (6,7,9,10); 4-MBC also penetrates a folioxane membrane, a model for human skin (8). Skin penetration may vary between compounds, as indicated by lower penetration of OMC as compared to Bp-3 (9,36), and appears to be influenced by the formulation (8,36).…”

Section: Discussionmentioning

confidence: 97%

In Vitro and in Vivo Estrogenicity of UV Screens

Schlumpf¹,

Cotton²,

Conscience³

et al. 2001

Environmental Health Perspectives

134

189

View full text Add to dashboard Cite

Estrogenic activity of UV filters determined by an in vitro reporter gene assay and an in vivo transgenic zebrafish assay

Schreurs

Lanser

Seinen

et al. 2002

Archives of Toxicology

165

View full text Add to dashboard Cite

In the past decade the list of chemicals in the environment that are able to mimic the natural hormone estrogen, thereby disrupting endocrine function, has grown rapidly. These chemicals are able to bind to estrogen receptors (ERs) and influence estrogen signalling pathways, although several of them have structures that differ substantially from the endogenous hormone 17beta-estradiol. In this study, six extensively used ultraviolet (UV) filters were assessed for transcriptional activation of estrogen receptors. Because of their high lipophilicity, these UV filters tend to bioaccumulate in the environment. They have been found in surface waters, fish, and in human milk fat. Using a sensitive in vitro reporter gene assay, we found that all six compounds induce estrogenic activity towards ERalpha, while four out of six compounds induced transcriptional activity of ERbeta. Zebrafish, in which an estrogen responsive luciferase reporter gene has been stably introduced, were used for in vivo testing. In this transgenic zebrafish assay none of the compounds showed estrogenic activity. Our findings suggest that one should be aware of over-interpretation when predicting in vivo effects from weak in vitro data. However, it can not be ruled out that these UV filters have long-term effects in the environment.

show abstract

Release of Benzimidazole and Benzylidene Camphor from Topical Sunscreen Formulations

Cited by 19 publications

References 7 publications

In vitro and in vivo estrogenicity of UV screens.

In vitro and in vivo estrogenicity of UV screens.

In Vitro and in Vivo Estrogenicity of UV Screens

Estrogenic activity of UV filters determined by an in vitro reporter gene assay and an in vivo transgenic zebrafish assay

Contact Info

Product

Resources

About