Betamethasone (9α-fluoro-16β-methyl-11β,17α,21-trihydroxy-1,4-pregnadiene-3,20-dione) is a synthetic glucocorticoid (GC). Some esters and salts of this compound are widely used as anti-inflammatory, immunosuppressive and antiproliferative agents, and also in dermatological therapy of different skin diseases. Despite minor differences in chemical structures, betamethasone derivatives may have different pharmacological effects. From the available literature it is obvious that the lipophilicity is one of many parameters which involved in biological activity of drugs including skin preparations [1,2]. This is a very important factor for their dermal permeation. Therefore, the main aim of this work was to determine the lipophilic properties of betamethasone and its derivatives: 17,21-dipropionate, betamethasone-17-valerate, betamethasone-21-valerate and also betamethasone disodium phosphate by means of reversed phase high performance thin-layer chromatography RP-HPTLC (R_MW) under different conditions, and also with the use of calculations (logP). All obtained results indicate that regardless of the applied method the biggest similarity in lipophilic properties show betamethasone-17-valerate, betamethasone-21-valerate and also betamethasone 17,21-dipropionate. Other betamethasone compounds indicate differences in lipophilicity parameters in mutual comparison.

Our study confirms that RP-HPTLC is a reliable, precise and cost-effective analytical tool which allows determining the lipophilicity of betamethasone and its related compounds.

1.  Jóźwiak, K.; Szumiło, H.; Soczewiński, E. Wiad. Chem. (in Polish), 2001, 55, (11/12), 1047-1074.

2.  Rutkowska, E.; Pająk, K.; Jóźwiak, K. Acta Pol. Pharm.-Drug Res. 2013, 70 (1), 3-18.

Acknowledgement:

This research was financed by the Medical University of Silesia as part of statutory research project in 2013 year, project No. KNW-1-013/N/3/0.

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1. TLC-Densitometric method for qualitative analysis of betamethasone and its related compounds in pharmaceutical preparations
2. Microarray analysis of CYP’s gene expression in human dermal fibroblasts with cyclosporine A