Abstract
The focus of the present work was to investigate the interaction of the anticancer drug mitoxantrone with two bile salts, sodium taurodeoxycholate (NaTDC) and sodium taurocholate (NaTC). Ultraviolet-visible (UV-Vis) absorption and electron paramagnetic resonance (EPR) spectroscopy were used to quantify the interaction and to obtain information on the location of mitoxantrone in bile salt micelles. The presence of submicellar concentrations of both bile salts induces mitoxantrone aggregation and the extent of drug aggregation in NaTDC is higher than in NaTC. For micellar bile salts concentrations, mitoxantrone monomers are entrapped in the micellar core. Binding constants, micelle/water partition coefficients and the corresponding thermodynamic parameters for binding and partitioning processes were estimated using the changes in monomer absorbance in the presence of bile salts. Binding interaction of mitoxantrone is stronger for NaTDC than NaTC micelles, whereas partitioning efficiency is higher for NaTC micelles for all investigated temperatures. Thermodynamic parameters indicate that both binding and partitioning processes are spontaneous and entropy controlled. The spectral behavior and thermodynamic parameters indicate distinct types of mitoxantrone interaction with NaTDC and NaTC micelles supported by the differences in nature and structure of bile salts micelles.
Highlights
Bile salts belong to the class of natural steroids and are synthesized in the liver and stored in the gallbladder
Mitoxantrone obtained in the presence of various NaTDC concentrations at 293.15 K temperature are shown in Figure 2, where it can be observed that the spectral absorption behavior of mitoxantrone is dependent on the NaTDC concentration
(a trihydroxy) bile salts has been investigated by combining UV-Vis absorption and electron paramagnetic resonance (EPR) spectroscopy techniques
Summary
Bile salts belong to the class of natural steroids and are synthesized in the liver and stored in the gallbladder. In addition to their biological role in digestion and gallstone formation, bile salts have received much attention as drug delivery systems and are used as membrane penetration enhancers in drug formulations [1,2,3,4,5]. Human bile salts differ in the number, position and stereochemistry of the hydroxyl groups as well as in the conjugated aminoacid, either taurine or glycine. The hydrophilic part of the bile salts is represented by the concave side of the rigid steroid ring system bearing the hydroxyl groups, while the hydrophobic part is represented
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