Alpha-monoisostearyl glyceryl ether enhances percutaneous penetration of indometacin in-vivo.
Molecules that reversibly remove the barrier resistance of skin enhance penetration. alpha-Monoisostearyl glyceryl ether (GE-IS) is a novel compound that can be used as a non-ionic surfactant and increases percutaneous penetration of indometacin in rat abdominal skin in-vitro. The present study investigated GE-IS-induced enhancement of indometacin penetration in-vivo. When 1% GE-IS in propylene glycol was applied to rat abdominal skin, serum and muscle concentrations of indometacin increased markedly. Anti-inflammatory activities of test solutions containing both indometacin and GE-IS were investigated in experimental models of acute and chronic inflammation. Application of indometacin with GE-IS to the skin produced greater inhibitory effects on carrageenan-induced rat paw oedema, UV-induced erythema in guinea-pigs, and adjuvant arthritis in rats, compared with application of indometacin alone. The results suggest that GE-IS enhances penetration in-vivo and improves the anti-inflammatory effects of indometacin in animal models. Thus, GE-IS might contribute to the development of cosmetic or medical formulations to improve transfer of bioactive substances to hypodermal sites.
Suzuki
Atsushi
A
Biological Science Laboratories, Kao Corporation, Tochigi, Japan.
Yamaguchi
Tatsuyuki
T
Kawasaki
Keiko
K
Hase
Tadashi
T
Tokimitsu
Ichiro
I
D000279:Administration, Cutaneous; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage / Q000493:pharmacokinetics*; D001169:Arthritis, Experimental / Q000188:drug therapy; D004487:Edema / Q000139:chemically induced / Q000188:drug therapy / Q000473:pathology; D004890:Erythema / Q000188:drug therapy; D005995:Glyceryl Ethers / Q000494:pharmacology*; D006168:Guinea Pigs; D007213:Indomethacin / Q000008:administration & dosage / Q000493:pharmacokinetics*; D008297:Male; D018482:Muscle, Skeletal / Q000187:drug effects / Q000502:physiology; D051381:Rats; D017207:Rats, Sprague-Dawley; D017208:Rats, Wistar; D012867:Skin / Q000187:drug effects; D012869:Skin Absorption / Q000187:drug effects*; D013501:Surface-Active Agents / Q000494:pharmacology*; D014466:Ultraviolet Rays
D000894:Anti-Inflammatory Agents, Non-Steroidal; D005995:Glyceryl Ethers; D013501:Surface-Active Agents; C439206:monoisostearyl glyceryl ether; D007213:Indomethacin