Methyl 2,5-dihydroxybenzoate

Dermal absorption

Administrative data

Endpoint:

dermal absorption in vitro / ex vivo

Type of information:

experimental study

Adequacy of study:

supporting study

Reliability:

2 (reliable with restrictions)

Rationale for reliability incl. deficiencies:

comparable to guideline study

Data source

Reference

Reference Type:

publication

Title:

Skin permeation and comparative evaluation of gentisic acid ester derivatives as skin-lightening agents

Author:

Nan Shun Ma, Marion Abraham, Myeong Jun Choi, Jung Sun Kim

Year:

2014

Bibliographic source:

J. DRUG DEL. SCI. TECH., 24 (2) 212-217 2014

Materials and methods

Principles of method if other than guideline:

Permeation through freshly excised mouse skin as tested in Franz diffusion cells at 37 °C for 12 hours.

GLP compliance:

no

Test material

Test material information

Constituent 1

Reference substance name:

Methyl 2,5-dihydroxybenzoate

EC Number:

218-427-8

EC Name:

Methyl 2,5-dihydroxybenzoate

Cas Number:

2150-46-1

Molecular formula:

C8H8O4

IUPAC Name:

methyl 2,5-dihydroxybenzoate

Test material form:

solid

Details on test material:

Synthesized by the authors of the publication. Identity confirmed by NMR and IR and melting point (2,5-dihydroxybenzoic acid methyl ester (MG)
m.p.: 85-87 °C (lit.: 84-86 °C); 1H NMR (CD3OD) δ: 4.84(s, 3H), 6.80(d, 1H), 6.96(dd, 1H), 7.21 (d, 1H); IR (KBr): 3338.36 cm-1 (O-H), 1685.26 cm-1 (C=O).

The product was purified by evaporation of the solvent, extraction with ethyl acetate, water and small aliquots of aqueous sodium bicarbonate until no gentisic acid was visible in the organic phase by thin layer chromatography. The organic layer was dried over sodium sulfate and evaporated in vacuum. A specific value for the purity was not reported in the publication.

Specific details on test material used for the study:

Temperature stability profiles of solutions of gentisic acid esters were determined over a time range of 12 h at 37 °C. No degradation of any gentisic acid analogues tested was observed within this time. Thus, the gentisic acid esters were stable at 37 °C for at least 12 h.

Radiolabelling:

no

Test animals

Species:

mouse

Strain:

not specified

Sex:

not specified

Details on test animals or test system and environmental conditions:

none provided

Administration / exposure

Type of coverage:

occlusive

Vehicle:

water

Duration of exposure:

12h

Doses:

supersaturated solution in water (Water solubility 27 mg/L)

No. of animals per group:

no data

Details on study design:

Samples were collected after 1, 2, 4,6, 8, 10 and 12 hours

Details on in vitro test system (if applicable):

SKIN PREPARATION
- Source of skin: mouse, freshly excised
- Type of skin: no data
- Preparative technique: no data
- Thickness of skin (in mm): no data
- Membrane integrity check: no data
- Storage conditions: not applicable
- Justification of species, anatomical site and preparative technique:

PRINCIPLES OF ASSAY
- Diffusion cell: Franz Cell
- Receptor fluid: 40 % (v/v) propylene glycol in buffered saline (PBS)
- Solubility od test substance in receptor fluid: soluble
- Static system: yes
- Test temperature: 37°C
- Occlusion: covered with parafilm

Results and discussion

Percutaneous absorption

Parameter:

rate

Remarks:

232 μg/cm2/h with lag time of 2.6 hours

Remarks on result:

other: linear increase in cumulative amount over 12hours

Applicant's summary and conclusion

Conclusions:

CAS 2150-46-1 permeates the skin.