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HPLC evaluation of solvolysis of a novel ester fluocinolone acetonide 21-(2'-phenoxypropionate) in comparison with fluocinonide

Authorized Users Only
2011
Authors
Marković, Bojan
Vladimirov, Sote
Čudina, Olivera
Savić, Vladimir
Karljiković-Rajić, Katarina
Article (Published version)
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Abstract
In this study the solvolysis of novel fluocinolone acetonide 21-(2'-phenoxypropionate) in comparison with fluocinonide was analyzed in order to evaluate this process as an in vitro model for prodrug activation. The solvolysis was performed in ethanol: water (90: 10 v/v) mixture using the excess of NaHCO3. The solvolytic mixtures of those esters with different lipophilicity were assayed by proposed RP-HPLC method using isocratic elution with methanol: water (75: 25 v/v); flow rate 1 mL min(-1), and detection at 238 nm. Solvolytic rate constants (at 25 degrees C) for novel prodrug fluocinolone acetonide 21-(2'-phenoxypropionate) (0.0434 h(-1)) and fluocinonide (0.0593 h(-1)) have been compared. This in vitro model of solvolysis and corresponding rate constants are in good correlation with our preliminary data of anti-inflammatory potencies of those prodrugs. Limits of detection, important for the initial stage of solvolysis, were experimentally determined with values of 4.10 mu M and 0.2...4 mu M for fluocinolone acetonide 21-(2'-phenoxypropionate) and fluocinonide, respectively.

Keywords:
fluocinolone acetonide esters / fluocinonide / prodrug / RP-HPLC / solvolysis / solvolytic rate constants
Source:
Journal of Liquid Chromatography & Related Technologies, 2011, 34, 19, 2271-2285
Publisher:
  • Taylor & Francis Inc, Philadelphia
Funding / projects:
  • Development of molecules with antiinflammatory and cardioprotective activity: structural modifications, modelling, physicochemical characterization and formulation investigations (RS-172041)

DOI: 10.1080/10826076.2011.587223

ISSN: 1082-6076

WoS: 000299376000003

Scopus: 2-s2.0-84855872884
[ Google Scholar ]
1
1
URI
https://farfar.pharmacy.bg.ac.rs/handle/123456789/1501
Collections
  • Radovi istraživača / Researchers’ publications
Institution/Community
Pharmacy
TY  - JOUR
AU  - Marković, Bojan
AU  - Vladimirov, Sote
AU  - Čudina, Olivera
AU  - Savić, Vladimir
AU  - Karljiković-Rajić, Katarina
PY  - 2011
UR  - https://farfar.pharmacy.bg.ac.rs/handle/123456789/1501
AB  - In this study the solvolysis of novel fluocinolone acetonide 21-(2'-phenoxypropionate) in comparison with fluocinonide was analyzed in order to evaluate this process as an in vitro model for prodrug activation. The solvolysis was performed in ethanol: water (90: 10 v/v) mixture using the excess of NaHCO3. The solvolytic mixtures of those esters with different lipophilicity were assayed by proposed RP-HPLC method using isocratic elution with methanol: water (75: 25 v/v); flow rate 1 mL min(-1), and detection at 238 nm. Solvolytic rate constants (at 25 degrees C) for novel prodrug fluocinolone acetonide 21-(2'-phenoxypropionate) (0.0434 h(-1)) and fluocinonide (0.0593 h(-1)) have been compared. This in vitro model of solvolysis and corresponding rate constants are in good correlation with our preliminary data of anti-inflammatory potencies of those prodrugs. Limits of detection, important for the initial stage of solvolysis, were experimentally determined with values of 4.10 mu M and 0.24 mu M for fluocinolone acetonide 21-(2'-phenoxypropionate) and fluocinonide, respectively.
PB  - Taylor & Francis Inc, Philadelphia
T2  - Journal of Liquid Chromatography & Related Technologies
T1  - HPLC evaluation of solvolysis of a novel ester fluocinolone acetonide 21-(2'-phenoxypropionate) in comparison with fluocinonide
VL  - 34
IS  - 19
SP  - 2271
EP  - 2285
DO  - 10.1080/10826076.2011.587223
ER  - 
@article{
author = "Marković, Bojan and Vladimirov, Sote and Čudina, Olivera and Savić, Vladimir and Karljiković-Rajić, Katarina",
year = "2011",
abstract = "In this study the solvolysis of novel fluocinolone acetonide 21-(2'-phenoxypropionate) in comparison with fluocinonide was analyzed in order to evaluate this process as an in vitro model for prodrug activation. The solvolysis was performed in ethanol: water (90: 10 v/v) mixture using the excess of NaHCO3. The solvolytic mixtures of those esters with different lipophilicity were assayed by proposed RP-HPLC method using isocratic elution with methanol: water (75: 25 v/v); flow rate 1 mL min(-1), and detection at 238 nm. Solvolytic rate constants (at 25 degrees C) for novel prodrug fluocinolone acetonide 21-(2'-phenoxypropionate) (0.0434 h(-1)) and fluocinonide (0.0593 h(-1)) have been compared. This in vitro model of solvolysis and corresponding rate constants are in good correlation with our preliminary data of anti-inflammatory potencies of those prodrugs. Limits of detection, important for the initial stage of solvolysis, were experimentally determined with values of 4.10 mu M and 0.24 mu M for fluocinolone acetonide 21-(2'-phenoxypropionate) and fluocinonide, respectively.",
publisher = "Taylor & Francis Inc, Philadelphia",
journal = "Journal of Liquid Chromatography & Related Technologies",
title = "HPLC evaluation of solvolysis of a novel ester fluocinolone acetonide 21-(2'-phenoxypropionate) in comparison with fluocinonide",
volume = "34",
number = "19",
pages = "2271-2285",
doi = "10.1080/10826076.2011.587223"
}
Marković, B., Vladimirov, S., Čudina, O., Savić, V.,& Karljiković-Rajić, K.. (2011). HPLC evaluation of solvolysis of a novel ester fluocinolone acetonide 21-(2'-phenoxypropionate) in comparison with fluocinonide. in Journal of Liquid Chromatography & Related Technologies
Taylor & Francis Inc, Philadelphia., 34(19), 2271-2285.
https://doi.org/10.1080/10826076.2011.587223
Marković B, Vladimirov S, Čudina O, Savić V, Karljiković-Rajić K. HPLC evaluation of solvolysis of a novel ester fluocinolone acetonide 21-(2'-phenoxypropionate) in comparison with fluocinonide. in Journal of Liquid Chromatography & Related Technologies. 2011;34(19):2271-2285.
doi:10.1080/10826076.2011.587223 .
Marković, Bojan, Vladimirov, Sote, Čudina, Olivera, Savić, Vladimir, Karljiković-Rajić, Katarina, "HPLC evaluation of solvolysis of a novel ester fluocinolone acetonide 21-(2'-phenoxypropionate) in comparison with fluocinonide" in Journal of Liquid Chromatography & Related Technologies, 34, no. 19 (2011):2271-2285,
https://doi.org/10.1080/10826076.2011.587223 . .

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