Open Accessα‐Monoisostearyl glyceryl ether enhances percutaneous penetration of indometacin in‐vivo
Author(s) -
Suzuki Atsushi,
Yamaguchi Tatsuyuki,
Kawasaki Keiko,
Hase Tadashi,
Tokimitsu Ichiro
Publication year - 2002
Publication title -
journal of pharmacy and pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.745
H-Index - 118
eISSN - 2042-7158
pISSN - 0022-3573
DOI - 10.1211/002235702342
Subject(s) - indometacin , in vivo , erythema , pharmacology , penetration (warfare) , chemistry , medicine , in vitro , surgery , biochemistry , enzyme inhibitor , prostaglandin endoperoxide synthase , microbiology and biotechnology , operations research , engineering , biology
Molecules that reversibly remove the barrier resistance of skin enhance penetration. α‐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.