Open Access
Rodriguez et al., J Chromatogr Sep Tech 2014, 5:5
DOI: 10.4172/2157-7064.1000244
Open Access Research Article
Volume 5 • Issue 5 • 1000244
J Chromatogr Sep Tech
ISSN: 2157-7064 JCGST, an open access journal
Development and Validation of a Liquid Chromatography Method with
Electrochemical Detection for Hydroxyurea Quantification in Human
Plasma and Aqueous Solutions
Anar Rodriguez
1
, Delphine Beukens
1
, Nicole Debouge
2
, Béatrice Gulbis
2
and Frédéric Cotton
1,2
*
1
Laboratory of Biological and Medical Chemistry, Faculty of Pharmacy, Université Libre de Bruxelles (ULB), Boulevard du Triomphe, 1050 Brussels, Belgium
2
Department of Clinical Chemistry, Erasme Hospital, Université Libre de Bruxelles, Route de Lennik 808 1070 Brussels, Belgium
*Corresponding author: Frédéric Cotton, Department of Clinical Chemistry,
Erasme Hospital, Université Libre de Bruxelles, 808 Route de Lennik - 1070
Brussels, Belgium, Tel: +3225553427; E-mail: fcotton@ulb.ac.be
Received September 18, 2014; Accepted September 22, 2014; Published
October 04, 2014
Citation: Rodriguez A, Beukens D, Debouge N, Gulbis B, Cotton F (2014)
Development and Validation of a Liquid Chromatography Method with
Electrochemical Detection for Hydroxyurea Quantifcation in Human Plasma
and Aqueous Solutions. J Chromatogr Sep Tech 5: 244. doi:10.4172/2157-
7064.1000244
Copyright: © 2014 Rodriguez A, et al. This is an open-access article distributed
under the terms of the Creative Commons Attribution License, which permits
unrestricted use, distribution, and reproduction in any medium, provided the
original author and source are credited.
Abstract
Hydroxyurea is the unique drug having demonstrated a signifcant effcacy in sickle cell disease treatment. We
developed a liquid chromatography method with electrochemical detection for hydroxyurea analysis in plasma and
aqueous solutions. Analytical goals included an analytical range from 2 to 50 mg/L, a total imprecision lower than
15% and a total error lower than 30%. After protein precipitation with acetonitrile, the separation was performed on a
C18 Atlantis T3 column and eluted with sodium acetate 25 mM, acetonitrile 2.5%, pH 6.5. Thioacetamide was used
as internal standard. The method was linear for drug concentrations ranging from 0.5 to 50 mg/L and recovery was
comprised between 100 and 120%. The intra-day precision was lower than 6.0% and between-day precision was
lower than 11%. The detection limit was 0.18 and 0.63 mg/L for aqueous solution and plasma, respectively and the
quantifcation limit was 1.0 and 1.2 mg/L for aqueous solution and plasma, respectively. No interference from urea
was observed. The liquid chromatography method developed can be used for pharmacokinetic studies in plasma
and other biological samples such as saliva or urine. It requires low sample volumes and a simple pre-treatment and
it allows a direct measure of non-derivatized hydroxyurea.
Keywords: Hydroxyurea; Hydroxycarbamide; Tioacetamide;
Liquid chromatography; Electrochemical detection; Sickle cell disease
Introduction
Hydroxycarbamide, better known as hydroxyurea, is a cytostatic
agent used in the treatment of myeloproliferative disorders such
as essential thrombocythemia and myelofbrosis [1,2]. It is also the
most active drug in sickle cell disease, a genetic disorder due to the
mutation of the 6th codon of the β-globin gene, leading to the synthesis
of an abnormal hemoglobin (Hb S); sickle cell disease is characterized
by chronic hemolytic anaemia and vaso-occlusive crises [3]. Te
main benefcial efect of hydroxyurea is to increase cellular levels of
fetal hemoglobin (Hb F), which reduces Hb S polymerization [4].
Others mechanisms were demonstrated or suggested such as reduced
expression of adhesion molecules, increased nitric oxide production,
cation transport changes and myelosuppressive efects [5,6].
Despite hydroxyurea therapy has shown clinical improvement for
sicke cell patients [7-9], diferences in response i.e., the increase in Hb
F levels, are observed and accurate predictors of hydroxyurea efcacy
do not currently exist [10]. When hydroxyurea is administrated orally
at a dose of 20 mg/kg, plasma concentrations normally reach a peak
within 2 h (T
max
) with a mean maximal concentration of 26 mg/L
(C
max
). Nevertheless, two phenotypes have recently been described: a
“fast” (T
max
of 15 or 30 min) and a “slow” one (T
max
of 60 or 120 min)
[10]. Pharmacokinetics studies are therefore required to explain these
diferences and to establish prediction factor.
Several methods have been developed to quantify hydroxyurea in
biological samples: colorimetric techniques [10], liquid chromatography
coupled with UV spectrophotometry [11,12], GC-MS [13,14], reversed
phase liquid chromatography coupled with mass spectrometry [15].
Colorimetric methods require sample volumes of 250-500 µL and are
insensitive. GC-MS needs a preliminary derivatization of hydroxyurea.
Here we describe the development and validation of a simple liquid
chromatography method with electrochemical detection to quantify
hydroxyurea in aqueous solutions and plasma.
Material and Methods
Chemicals and pre-analytical treatment
A stock solution of hydroxyurea (Sigma Aldrich, Steinheim,
Germany) at 1000 mg/L was prepared and kept at -20°C. Aqueous and
plasma standards were prepared by dilution of the stock solution in
distilled water or human plasma pool.
Tiourea, methylurea, 2-thiouracil and thioacetamide (Sigma
Aldrich, Steinheim, Germany) were tested as internal standard. Te
solutions were prepared at a fnal concentration of 100 mg/L containing
3 g/L albumin (Behring Institut, Marburg, Germany).
10 µL of samples or standards were added with 10 µL of internal
standard solution and 100 µL acetonitrile (Biosolve, Dieuze, France).
Afer centrifugation at 4000 rpm during 10 minutes, 80 µL of
supernatant were recovered and either diluted to 400 µL with mobile
phase or dried under nitrogen and reconstituted in 400 µL of mobile
phase.
Two mobile phases were tested. Te frst one was described by
Pujari and collaborators [16] and was composed of 0.2 M perchlorate
and methanol 95/5 (V/V) (Sigma Aldrich, Steinheim, Germany). Te
Journal of Chromatography
Separation Techniques
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ISSN: 2157-7064