Anti-inflammatory effects of methylprednisolone aceponate in animals

• Published in: Nihon yakurigaku zasshi Vol. 98; no. 5; p. 409
• Main Authors: Ikoma, Y, Yamashita, M, Kamitani, K, Nakagawa, H
• Format: Journal Article
• Language: Japanese
• Published: Japan 1991
• Subjects: Administration, Topical; Animals; Anti-Inflammatory Agents - pharmacology; Anti-Inflammatory Agents - therapeutic use; Croton Oil; Edema - chemically induced; Edema - drug therapy; Female; Granuloma - drug therapy; Hypersensitivity, Delayed - drug therapy; Injections, Subcutaneous; Male; Methylprednisolone - pharmacology; Methylprednisolone - therapeutic use; Mice; Rats; Rats, Inbred Strains; Skin Diseases - drug therapy
• ISSN: 0015-5691
• DOI: 10.1254/fpj.98.5_409

In the case of dermal application of the drugs to croton oil-induced ear edema in rats and picryl chloride-induced delayed type hypersensitivity in mice, the anti-inflammatory effect of methylprednisolone aceponate (MPA) was slightly weaker than those of clobetasol 17-propionate and diflucortolone 21-valerate, but stronger than those of hydrocortisone 17-butyrate and hydrocortisone 17-butyrate 21-propionate. Betamethasone 17-valerate applied dermally was less and more effective than MPA to ear edema in rats and delayed type hypersensitivity in mice, respectively. The anti-inflammatory effect of MPA was weaker in subcutaneous administration than in topical application to the two inflammatory models. It was suggested that MPA has strong anti-inflammatory effects and weak systemic effects by topical application. Methylprednisolone 17-propionate (MP-17P) and methylprednisolone (MP), unesterified in only the C-21 position and in both the C-17 and 21 positions of MPA, respectively, showed weaker anti-inflammatory activities than MPA by topical application to croton oil-induced ear edema. The ratio of the anti-inflammatory effects by topical application to subcutaneous administration of MPA was higher than those of MP-17P and MP. The excellent characteristics of MPA as a dermal anti-inflammatory drug are suggested to be derived from di-esterification of MP, which has a weak activity intrinsically.