Enhancing effect of alpha-monoisostearyl glyceryl ether on the percutaneous penetration of indomethacin through excised rat skin.
The enhancing effect of alpha-monoisostearyl glyseryl ether (GE-IS) on the percutaneous penetration of indomethacin (IM) from test solutions in propylene glycol (PG) was investigated using the excised abdominal skin of rats in vitro. The percutaneous penetration of IM into diffusion cells was significantly increased in the presence of 0.2% or 1% (w/w) GE-IS compared with enhancer-free PG solution. Permeation parameters of IM, such as lag time and permeability coefficient, revealed that GE-IS significantly augmented the percutaneous penetration of IM from PG. These results strongly suggested that GE-IS functions as a penetration enhancer of IM through rat skin. To elucidate the mode of action of GE-IS as a penetration enhancer, the solubility of IM in the test solution and the percutaneous penetration of IM through damaged skin from which the stratum corneum had been stripped were investigated. The results suggested that GE-IS acts directly on the stratum corneum and alters the permeability of the skin.
Suzuki
A
A
Biological Science Laboratories, Kao Co., Tochigi, Japan.
Yamaguchi
T
T
Kawasaki
K
K
Hase
T
T
Tokimitsu
I
I
D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000493:pharmacokinetics*; D005995:Glyceryl Ethers / Q000494:pharmacology*; D066298:In Vitro Techniques; D007213:Indomethacin / Q000493:pharmacokinetics*; D008297:Male; D051381:Rats; D012869:Skin Absorption / Q000187:drug effects*
D000894:Anti-Inflammatory Agents, Non-Steroidal; D005995:Glyceryl Ethers; C439206:monoisostearyl glyceryl ether; D007213:Indomethacin