Lipophilic copper(II) formulations: some correlations between their composition and anti-inflammatory/anti-arthritic activity when applied to the skin of rats.
Copper complexes of phenols related to salicylic acid were prepared in DMSO and applied to the shaved dorsal skin of rats. The following activities were assayed: (i) suppression of the carrageenan or hydroxylapatite paw oedemas; (ii) reduction of chronic inflammation in established adjuvant arthritis; (iii) local skin toxicity. Cu(II) was an essential component. Some limited structure-activity correlations were made among alternative cupriphores. DMSO solutions of copper complexes were more potent than their solutions in ethanol. Glycerol was a beneficial additive. Reducing the acidity of some copper salicylate formulations also reduced their potency. Niflumic acid and phenylbutazone were effective non-salicylate transcutaneous cupriphores.
D000287:Administration, Topical; D000818:Animals; D000893:Anti-Inflammatory Agents; D001169:Arthritis, Experimental / Q000188:drug therapy; D003300:Copper / Q000008:administration & dosage / Q000494:pharmacology*; D007501:Iron / Q000494:pharmacology; D008024:Ligands; D051381:Rats; D011919:Rats, Inbred Strains; D012459:Salicylates / Q000008:administration & dosage; D012869:Skin Absorption; D015032:Zinc / Q000494:pharmacology
D000893:Anti-Inflammatory Agents; D008024:Ligands; D012459:Salicylates; D003300:Copper; D007501:Iron; D015032:Zinc