Acyloxyamines as prodrugs of anti-inflammatory carboxylic acids for improved delivery through skin.
An N,N-dialkylhydroxylamine derivative of indomethacin has been synthesized. It has been shown to improve the delivery of indomethacin through mouse skin (compared to indomethacin itself) by a factor of two, to be more effective than indomethacin in inhibiting thermal inflammation (two to three times) in animal models, but to be only as effective as indomethacin in inhibiting UV-B radiation erythema in human volunteers.
D000287:Administration, Topical; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000138:chemical synthesis* / Q000378:metabolism; D002056:Burns / Q000188:drug therapy / Q000378:metabolism; D002264:Carboxylic Acids / Q000378:metabolism* / Q000627:therapeutic use; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D004058:Diffusion; D006801:Humans; D006898:Hydroxylamines / Q000008:administration & dosage / Q000138:chemical synthesis* / Q000378:metabolism; D007213:Indomethacin / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000378:metabolism / Q000627:therapeutic use; D051381:Rats; D012869:Skin Absorption; D013471:Sunburn / Q000188:drug therapy / Q000378:metabolism
D000893:Anti-Inflammatory Agents; D002264:Carboxylic Acids; D006898:Hydroxylamines; D007213:Indomethacin