Effects of sucrose oleate and sucrose laureate on in vivo human stratum corneum permeability.
OBJECTIVE
The purpose of this work was to 1) investigate the effect of sucrose esters (sucrose oleate and sucrose laureate in water or in Transcutol, TC) on the stratum corneum (SC) barrier properties in vivo and 2) examine the impact of these surfactant-like molecules on the in vivo percutaneous penetration of a model penetrant 4-hydroxybenzonitrile (4-HB).


METHODS
Attenuated total reflectance Fourier transform infrared (ATR-FTIR) spectroscopy and transepidermal water loss measurements were used to evaluate the sucrose oleate- and sucrose laureate-induced biophysical changes in SC barrier function in vivo. In addition. the effect of the enhancers on 4-HB penetration was monitored in vivo using ATR-FTIR spectroscopy in conjunction with tape-stripping of the treated site.


RESULTS
Treatment of the skin with 2% sucrose laureate or sucrose oleate in TC significantly increased the extent of 4-HB penetration relative to the control. Furthermore, when skin treated with these formulations was examined spectroscopically, the C-H asymmetric and symmetric stretching bands of the lipid methylene groups were characterized by 1) decreased absorbances and 2) frequency shifts to higher wavenumbers. These effects on the SC lipids and 4-HB penetration were more pronounced for sucrose laureate when combined with TC.


CONCLUSIONS
A combination of sucrose esters (oleate or laureate) and TC is able to temporally alter the stratum corneum barrier properties, thereby promoting 4-HB penetration. These molecules are worthy of further investigation as potential candidates for inclusion in transdermal formulations as penetration enhancers.
Ayala-Bravo
Hilda A
HA
División de Estudios de Posgrado (Tecnología Farmacéutica), Facultad de Estudios Superiores Cuautitlan/Universidad Nacional Autónoma de México, Av. 1 de Mayo s/n, Cuautitlán Izcalli, Estado de México, México 54704.
Quintanar-Guerrero
David
D
Naik
Aarti
A
Kalia
Yogeshvar N
YN
Cornejo-Bravo
José M
JM
Ganem-Quintanar
Adriana
A
D000328:Adult; D004817:Epidermis / Q000187:drug effects* / Q000378:metabolism; D004952:Esters; D005260:Female; D006801:Humans; D008954:Models, Biological; D010539:Permeability; D014677:Pharmaceutical Vehicles; D010636:Phenols / Q000493:pharmacokinetics; D012869:Skin Absorption / Q000187:drug effects*; D012995:Solubility; D017550:Spectroscopy, Fourier Transform Infrared; D013395:Sucrose / Q000031:analogs & derivatives* / Q000494:pharmacology*
D004952:Esters; D014677:Pharmaceutical Vehicles; D010636:Phenols; C007178:4-cyanophenol; D013395:Sucrose