M.S. Nesterov
Head of Laboratory for Bioanalytical Research,
Scientific Center of Biomedical Technologies of the Federal Medical and Biological Agency of Russia
(Moscow region, Krasnogorsk district, pos. Bright mountains, Russia)
D.V. Khvostov
Junior Research Scientist, Laboratory of Molecular Biology and Bioinformatics,
V.M. Gorbatov Federal Research Center for Food Systems, Russian Academy of Sciences (Moscow, Russia)
R.A. Ageldinov
Research Scientist, Laboratory for Bioanalytical Research,
Scientific Center of Biomedical Technologies of the Federal Medical and Biological Agency of Russia
(Moscow region, Krasnogorsk district, pos. Bright mountains, Russia)

Methylprednisolone aceponate (MPA) is potent (class III) topical corticosteroid widely used for the treatment of inflammatory dermatoses. It’s peculiari-ties are exceptionally favorable safety profile, high anti-inflammatory activity and properties of prodrug – after application to the skin MPA is trans-formed into active metabolite methylprednisolone 17-propionate, and this process goes more intensively in the zone of inflammation thus limiting ster-oid effect on intact skin. After the patent expiration generic MPA drugs which didn’t pass through the full cycle of clinical trials have entered some markets, including Russian. Metabolic profile of these generics and it’s equivalence to the original product is unknown. Objective. To assess biological activity of various drug formulations of original (Advantan®) and generic (Komfoderm®) drugs of MPA using vasocon-striction assay in the in vivo model. Methods. Recommended doses of studied formulations were applied to the skin of laboratory animals (mini-pigs), and then experimental measure-ments of chromometric data were performed at specific timepoints (0.5 h, 3h, 6 h, 12 h, 24 h) using chromometer FRU WR-10 (8 mm). Results. Difference in the profile of biologic activity based on vasoconstriction assay data was noticed for all tested MPA drugs, ranging in descending order for lightness parameter L: Advantan® cream – Advantan® milk – Advantan® fatty ointment – Advantan® ointment – Komfoderm® К cream – Komfoderm® ointment – Komfoderm ® М2 ointment. Conclusions. Applicability of colorimetric method for evaluation of intensity of biologic effect of glucocorticoids based on the level of lightness of skin surface confirmed. Differences for this parameter for studied drugs detected. Noticed tendency to higher activity of the original drug in comparison to the generic.

methylprednisolone aceponate
referent drug
vasoconstriction assay

  1. Левина Ю.Г., Алексеева А.А., Вишнева Е.А. и др. Осо-бенности наружной терапии атопического дерматита у детей: роль метилпреднизолона ацепоната. Педиатрическая фармакология. 2014; 11(5): 52–58. doi: 10.15690/pf.v11i5.1165 (Levina Ju.G., Alekseeva A.A., Vishneva E.A. i dr. Osobennosti naruzhnoj terapii atopicheskogo dermatita u detej: rol' metilprednizolona aceponata. Pediatricheskaja farmakologija. 2014; 11(5): 52–58. doi: 10.15690/pf.v11i5.1165).
  2. Ruzicka T. Methylprednisolone aceponate in eczema and other in-flammatory skin disorders – a clinical update. Int. J. Clin. Pract. 2006; 60(1): 85–92. doi: 10.1111/j.1368-5031.2005.00754.x.
  3. Zaumseil R.P., Fuhrmann H., Kecskes A., et al. Methylpredniso-lone aceponate (Advantan) – an effective topical corticoid therapy with few side effects. (In German). Jahrb. Dermatol. 1992; 3: 247–263.
  4. Fritsch P. Clinical experience with methylprednisolone aceponate (MPA) in eczema. J. Dermatolog. Treat. 1992; 3(Suppl. 2): 17–19. doi:10.3109/09546639209092768.
  5. Luger T., Loske K.D., Elsner P., et al. Topical skin therapy with glucocorticoids-therapeutic index. (In German). J. Dtsch. Dermatol. Ges. 2004; 2(7): 629–634.
  6. Волкова Е.Н., Ланге Д.А., Родина Ю.А., Тарасова М.В. Метилпреднизолона ацепонат в комплексной терапии хронических дерматозов: анализ тактических ошибок применения. Клиническая дерматология и венерология. 2010; 5: 97–102 (Volkova E.N., Lange D.A., Rodina Ju.A., Tarasova M.V. Metilprednizolona aceponat v kompleksnoj terapii hronicheskih dermatozov: analiz takticheskih oshibok primenenija. Klinicheskaja dermatologija i venerologija. 2010; 5: 97–102).
  7. Blume-Peytavi U., Wahn U. Optimizing the treatment of atopic dermatitis in children: a review of the benefit/risk ratio of methylprednisolone aceponate. J. Eur. Acad. Dermatol. Venereol. 2011; 25(5): 508–515. doi: 10.1111/j.1468-3083.2010.03942.x.
  8. Нестеров М.С., Хвостов Д.В., Агельдинов Р.А. Результаты сравнительного метаболического анализа наружных лекар-ственных препаратов метилпреднизолона ацепоната in vivo. Врач. 2021; 32 (7): 86–92. doi: 10.29296/25877305-2021-07-15 (Nesterov M.S., Hvostov D.V., Agel'dinov R.A. Rezul'taty sravnitel'nogo metabolicheskogo analiza naruzhnyh lekarst-vennyh preparatov metilprednizolona aceponata in vivo. Vrach. 2021; 32 (7): 86–92. doi: 10.29296/25877305-2021-07-15).
  9. Andersen P.H., Bjerring P. Noninvasive computerized analysis of skin chromophores in vivo by reflectance spectroscopy. Photoder-matol Photoimmunol Photomed. 1990; 7: 249–57.
  10. Baquie M., Kasraee B. Discrimination between cutaneous pigmen-tation and erythema: comparison of the skin colorimeters Derma-catch and Mexameter. Skin Res. Technol. 2014; 20(2): 218–27.
  11. International Color Consortium, Specification ICC.1:2004–10 (Pro-file version Image technology colour management – archi-tecture, profile format, and data structure. 2006.
  12. Westerhof W. CIE colorimetry. In: Serup J., Jemec G.B.E., editors. Handbook of non-invasive methods and the skin. Boca Raton: CRC Press; 1995: 385–97.
  13. Takiwaki H. Measurement of skin color: practical application and theoretical considerations. J. Med. Invest. 1998; 44: 121–6.
  14. Queille-Roussel C., Pocet M., Scaffer H. Quantification of skin col-our changes induced by topical corticosteroid preparations using the Minolta Chroma Meter. Br. J. Dermatol. 1991; 124: 264–270.
  15. Dermatological and Transdermal Formulations. Edited by Kenneth A. Walters. 2002; 592 p.
  16. Guidance for Indusrty: Topical-Dermatologic Corticosteroids: in-Vivo-Bioequivalence. 1995.
  17. McKenzie A.W., Stoughton R.B. Method for comparing percutane-ous absorption of steroids. Arch Dermatol. 1962; 86: 608–10.
  18. Coldman M.F., Lockerbie L., Laws E.A. The evaluation of several topical corticosteroid preparations in the blanching test. Br J Derma-tol. 1971; 85: 381–387.
  19. Heseltine W.W., McGilchrist J.M., Gartside R. Comparative vaso-constrictor activities of corticosteroids applied topically. Br. J. Der-matol. 1964; 76:71–73.
  20. Clanachan I., Devitt H.G., Foreman M.I., et al. The human vaso-constrictor assay for topical steroids. J. Pharmacol. Method. 1980; 4: 209–20.
  21. FDA Guidance for industry: DraftTopical dermatological drug products NDAs and ANDAs in vivo bioavailability and bioe-quivalence. In vitro studies and associated studies. 1998.
  22. Barry B.W., Woodford R. Activity and bioavailability of topical cor-ticosteroids: in vivo/in vitro correlations for the vasoconstrictor test. J. Clin. Pharm. 1978; 3: 43–65.
  23. Haigh J.M., Kanfer I. Assessment of topical corticosteroid prepara-tions: the human skin blanching assay. Int. J. Pharm. 1984; 19: 24562