Octocrilene

Dermal absorption

Administrative data

Endpoint:

dermal absorption

Type of information:

experimental study

Adequacy of study:

weight of evidence

Study period:

no data

Reliability:

2 (reliable with restrictions)

Rationale for reliability incl. deficiencies:

study well documented, meets generally accepted scientific principles, acceptable for assessment

Data source

Reference

Reference 1

Reference Type:

study report

Title:

Unnamed

Year:

1998

Report date:

1998

Reference 2

Reference Type:

study report

Title:

Unnamed

Year:

1998

Report date:

1998

Materials and methods

Test guideline

Qualifier:

equivalent or similar to guideline

Guideline:

OECD Guideline 428 (Skin Absorption: In Vitro Method)

Principles of method if other than guideline:

In vitro penetration studies using human and porcine skin

GLP compliance:

not specified

Test material

Test material information

Constituent 1

Reference substance name:

Octocrilene

EC Number:

228-250-8

EC Name:

Octocrilene

Cas Number:

6197-30-4

Molecular formula:

C24H27NO2

IUPAC Name:

2-ethylhexyl 2-cyano-3,3-diphenylacrylate

Details on test material:

- Name of test material (as cited in study report): Uvinul N 539
No further data

Radiolabelling:

no

Test animals

Species:

other: pig and human

Administration / exposure

Vehicle:

other: oil water emulsion

Duration of exposure:

16 hours

Doses:

3 mg/cm² (8% test substance)

Details on in vitro test system (if applicable):

Human Skin
SKIN PREPARATION
- Type of skin: Human caucasian skin from mammalian or abdominal surgery of females aged between 20 and 65 years
- Preparative technique: freshly dermatomed
- Thickness of skin: 350 ± 50 µm
- Membrane integrity check: yes: visually (no cuts, scars, reddish marks, spots, injuries), TEWL
- Storage conditions: 4°C for 24 hours

PRINCIPLES OF ASSAY
- Diffusion cell: static
- Receptor fluid: 1% of bovine serum albumin, 0.9 % of NaCl, 0.02 % of KCI, 0.04 % of gentamicin sulfate and 0.8% of phosphate buffer in water; pH 7.4.
- Test temperature: mean skin membrane temperature of 32 °C
- Samples assessed: Tapes (16 strippings); epidermis, dermis, receptor fluid, washing solution

Pig Skin
SKIN PREPARATION
- Type of skin: Unboiled back skin of selected female pigs ( 130 days old, weighing about 100 kg). Fresh skin from 6 different animals was used in triplicate.
- Preparative technique: freshly dermatomed
- Thickness of skin: 700 ± 50 µm
- Membrane integrity check: yes: visually (no cuts, scars, scratches, injuries), TEWL

PRINCIPLES OF ASSAY
- Diffusion cell: static
- Receptor fluid: 1% of bovine serum albumin, 0.9 % of NaCl, 0.02 % of KCI, 0.04 % of gentamicin sulfate and 0.8% of phosphate buffer in water; pH 7.4.
- Test temperature: mean skin membrane temperature of 32 °C
- Samples assessed: Tapes (16 strippings); epidermis, dermis, receptor fluid, washing solution

Results and discussion

Total recovery:

Pig skin experiments: 90+/-2% recovery

Percutaneous absorption

Percutaneous absorption 1

Time point:

16 h

Dose:

3 mg/cm²

Parameter:

percentage

Absorption:

ca. 0.2 %

Remarks on result:

other: Human Skin: Application of test substance as 8% in formulation

Percutaneous absorption 2

Time point:

16 h

Dose:

3 mg/cm²

Parameter:

percentage

Absorption:

ca. 3 %

Remarks on result:

other: Porcine Skin: Application of test substance as 8% in formulation

Any other information on results incl. tables

Pig skin - Distribution of the total amount of Caffeine and Uvinul N 539 in six skin samples

Mean % of applied amount (confidence interval of 95%)

	Octocrilene Uvinul N539	Caffeine
Surface	74 (4)	83 (2)
Stratum corneum	14 (3)	5.0 (1)
Epidermis	2.8 (0.9)	3.0 (1)
Dermis	0.3 (0.1)	1.0 (0.5)
Receptor medium	0.0 (0)	0.6 (0.4)
Recovery	90 (2)	93 (4)

Caffeine	% of applied dose
	skin 1	skin 2	skin 3	skin 4	skin 5	skin 6
loss	3.28	7.56	9.39	4.35	6.88	9.37
surface	92.63	89.19	82.31	85.26	84.16	82.24
SC	1.91	1.09	4.85	5.49	3.82	4.72
epidermis	0.64	1.28	2.12	2.12	3.38	1.99
dermis	0.65	0.39	0.78	1.41	1.13	0.69
receptor	0.89	0.49	0.45	0.36	0.64	0.98

Uvinul N 539	% of applied dose
	skin 1	skin 2	skin 3	skin 4	skin 5	skin 6
loss	8.04	10.47	7.15	10.12	10.96	10.82
surface	75.02	75.53	72.9	73.37	67.38	76.98
SC	13.78	10.83	15.15	14.3	18.89	9.8
epidermis	2.78	2.95	4.34	2	2.4	1.03
dermis	0.38	0.22	0.46	0.21	0.39	0.37
receptor	0	0	0	0	0	0

Comparison between the repartition profiles in pig an human skin

skin compartment	µg of applied substance per cm² skin
	Caffeine		Octocrilene Uvinul N 539
	pig n = 12	human n = 12	pig n = 18	human n = 9
surface	139 ± 12	82 ± 7	157 ± 15	216 ± 17
SC	8 ± 2	2 ± 2	30 ± 8	13 ± 6
epidermis	4 ± 2	0.13 ± 0.08	6 ± 2	0.3 ± 0.7
dermis	1.7 ± 0.9	0.3 ± 0.2	0.7 ± 0.2	0.3 ± 1.0
receptor	1.0 ± 0.6	1.4 ± 0.9	0.0 ± 0.0	0.0 ± 0.0

Considering the concentration of the test substance (8%) and the amount applied (3 mg/cm²), 5.4%, 0.125% and 0.125% of the applied dose was found in human stratum corneum, epidermis and dermis respectively. No octocrilene was detectable in the receptor fluid.