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Investigation of solvolysis kinetics of new synthesized fluocinolone acetonide C-21 esters--an in vitro model for prodrug activation.

Markovic, Bojan D; Dobricic, Vladimir D; Vladimirov, Sote M; Cudina, Olivera A; Savic, Vladimir M; Karljikovic-Rajic, Katarina D.
Molecules; 16(3): 2658-71, 2011 Mar 23.
Artículo en Inglés | MEDLINE | ID: mdl-21441868
In this study the solvolysis of newly synthesized fluocinolone acetonide C-21 esters was analysed in comparison with fluocinonide during a 24-hour period of time. The solvolysis was performed in an ethanol-water (9010 v/v) mixture using the excess of NaHCO3. The solvolytic mixtures of each investigated ester have been assayed by a RP-HPLC method using isocratic elution with methanol-water (7525 v/v); flow rate 1 mL/min; detection at 238 nm; temperature 25 °C. Solvolytic rate constants were calculated from the obtained data. Geometry optimizations and charges calculations were carried out by Gaussian W03 software. A good correlation (R = 0.9924) was obtained between solvolytic rate constants and the polarity of the C-O2 bond of those esters. The established relation between solvolytic rate constant (K) and lipophilicity (cLogP) with experimental anti-inflammatory activity could be indicative for topical corticosteroid prodrug activation.