Effect of Crystal Form on in Vivo Topical Anti-Inflammatory Activity of Corticosteroids

  • Published : 2002.08.01


The aim of this study was to gain information on the effects of the crystal form of corticosteroids on the topical anti-inflammatory activity. Two different crystal forms, Form A and Form B, of the drugs of prednicarbate, hydrocortisone, betamethasone 17-valerate, prednisolone, and methyl prednisolone were prepared and their topical anti-inflammatory activities were measured using arachidonic acid induced ear edema assay in mice. Two crystal forms of the drugs showed differences in anti-inflammatory activity. Among the drugs examined, Form B of prednicarbate and betamethasone 17-valerate showed significantly more potent anti-inflammatory activities as compared to their Form A.


  1. Idson, B., Vehicle effects in percutaneous absorption. Drug Metab. Rev., 14, 207-222 (1983) https://doi.org/10.3109/03602538308991389
  2. Massimo, F. and Giovanni, P., Corticosteroid dermal delivery with skin-lipid liposomes. J. Controlled ReI., 44, 141-151 (1997) https://doi.org/10.1016/S0168-3659(96)01519-2
  3. Buyuktimkin, N., Buyuktimkin, S. and Rytting, J. H., Chemical means of transdermal drug permeation enhancement. In Ghosh, T. K., Pfister, W. R. and Yum, S. I. (Eds.).Transdermal and topical drug delivery systems, Interpharm PressInc., Buffalo Grove, Illinois, pp.357, (1997)
  4. Green, P. G., Flanagan, M., Shroot, B. and Guy, R. H., Iontophoretic Drug Delivery. In Walters, K.A. and Hadgraft, J. (Eds.). Pharmaceutical skin penetration enhancement, Marcel Decker, New York, pp.331, (1993)
  5. Prausnitz, M. R., Pliquett, U., Langer, R. and Weaver, J. C., Rapid temporal control oftransdermal drug delivery by electroporation. Pharm. Res., 11, 1834-1837 (1994) https://doi.org/10.1023/A:1018944223290
  6. Murphy, T. M. and Hardgraft, J. A., Physicochemical interpretation of phonoporesis in skin penetration enhancement. In Scott, R. C., Guy, R. H. and Hardgraft, J. (Eds.). Prediction percutaneous penetration: methods, measurements, modeling, IBC Technical Service Ltd., London, pp 333, (1990)
  7. Watson, W. S. and Finlay, A. Y., The effect of the vehicle formulation on the stratum corneum penetration characteristics of clobetasoI 17-propionate. Br. J. Dermatol., 118, 523-530 (1988) https://doi.org/10.1111/j.1365-2133.1988.tb02462.x
  8. Bird, J., Kim, H. P. and Lee, H. J., Anti-inflammatory activity of esters of steroid 21-oicacids. Steroids, 47, 35-40 (1986) https://doi.org/10.1016/0039-128X(86)90074-7
  9. Kim, H. K., Namgoong, S. Y. and Kim, H. P., Anti-inflammatory activity of flavonoids:Mouse ear edema inhibition. Arch. Pharm. Res., 16, 18-24 (1993) https://doi.org/10.1007/BF02974122
  10. Mesley, R. J., The infra-red spectra of certain steroids and dissolution rate of their tablets. Spectrochim. Acta, 22, 889-917 (1966) https://doi.org/10.1016/0371-1951(66)80119-4
  11. Gao, C. K. and Zahng, R. H., Polymorphic forms of certain steroids and dissolution rate of their tablets. Pharm. Ind., 18, 301-306 (1987)
  12. De Maury; G., Chauvet; A., Terol, A. and Masse, J., Etude thermoanalytique de quelques steroids IV. Prednisolone etderives. Thermochimica Acta, 97, 127-142 (1986) https://doi.org/10.1016/0040-6031(86)87014-9
  13. Veiga, M. D., Cadomiga, R., Fonseca, I. and Garcia-Blanco, S., Polymorphism characterization of prednisolone: spectrometric and diffractometric study. II Farmaco Ed. Pr., 42, 93-102 (1987)
  14. Guillory, J. K., Heat of transition of methylprednisolone and sulfathiazole by a differential thermal analysis method. J. Pharm. Sci., 56, 72-76 (1967) https://doi.org/10.1002/jps.2600560115