Developing an Analytical Method Based on Graphene Quantum Dots for Quantification of Deferiprone in Plasma.

In the world of nanotechnology, graphene quantum dots (GQDs) have been considerably employed in numerous optical sensing and bioanalytical applications. Herein, a simple and cost-efficient methodology was developed to the quantification of deferiprone in plasma samples by utilizing the selective interaction of the GQDs and drug in the presence of Fe3+ ions. GQDs were synthesized by a bottom-up technique as an advantageous fluorescent probe. Increasing levels of deferiprone ranging from 5 to 50 mg.L-1, leads to significant fluorescence quenching of GQDs. In addition, the calibration curve was revealed a linear response in this range with a sensitivity of 5 mg.L-1. The method validation was carried out according to the FDA guidelines to confirm the accuracy, precision, stability and selectivity of the developed method. The results show that this green and low-cost fluorescent probe could be used for the analysis of deferiprone.

A ratiometric fluorometric and colorimetric probe for the ß-thalassemia drug deferiprone based on the use of gold nanoclusters and carbon dots.

A turn-on fluorometric probe is described for the ß-thalassemia drug deferiprone (DFP). The probe is making use of carbon dots (C-dots) and gold nanoclusters (AuNCs) which, under 340-nm excitation, display dual emission with peaks at 445 and 592 nm. The orange fluorescence of AuNCs is quenched after the addition of Fe(III), but recovered on addition of DFP. The blue fluorescence of the C-dots, in contrast, remains unchanged. The Fe(III)-DFP complex undergoes intermolecular electron transfer under UV excitation and displays only weak peaks in the UV region. The ratio of the two fluorescences is measured which makes the probe intrinsically self-calibrated. Colorimetry is best performed at a wavelength of 280 nm. The ratio of fluorescences increases linearly in the 0.1-80 µM DFP concentration range, and the detection limit is 0.1 µM. The respective figures for colorimetry are 2.5-120 µM and 0.3 µM. The probe is highly selective for DFP. Thus, it possesses a large potential for detection of DFP in serum. Graphical abstract The orange fluorescence of gold nanoclusters (AuNCs) is quenched by Fe3+ ions but recovered on addition of deferiprone (DFP), while the change of blue fluorescence in carbon dots (C-dots) is minimal. Moreover, the Fe(III)-DFP complex undergoes intermolecular electron transfer under ultraviolet (UV) irradiation, and absorption spectra can be observed in the presence of Fe(III)-DFP detected by UV scanning. Thus, a ratiometric fluorometric and colorimetric assay is developed for DFP.

Randomized, Blinded, Placebo- and Positive-Controlled Crossover Study to Determine the Effect of Deferiprone on the QTc Interval in Healthy Subjects.

This study evaluated whether deferiprone, an oral iron chelator, acts to prolong the QT interval. Fifty healthy volunteers received single doses of each of the following: therapeutic dose of deferiprone (33 mg/kg), supratherapeutic dose (50 mg/kg), placebo, or moxifloxacin, a positive control known to significantly prolong QT interval. Following each dose, subjects underwent cardiac monitoring, pharmacokinetics assessments, and safety assessments. Based on the QT interval obtained using the Fridericia correction for heart rate (QTcF), the upper bound of the 1-sided 95% confidence interval of the mean difference between deferiprone and placebo was <10 milliseconds (the threshold of concern defined by authorities) at all time points for both doses: maximum difference of 3.01 milliseconds for the therapeutic dose and 5.23 milliseconds for the supratherapeutic dose. The difference in dQTcF between moxifloxacin and placebo demonstrated that the study was adequately sensitive to detect a significant prolongation of QTcF. The concentration-response correlation analyses revealed some weak but statistically significant trends of increase in dQTcF and ddQTcF with increasing exposure to deferiprone, but these trends should have no clinical consequence even at the recommended maximum dosage. In conclusion, there was no clinically meaningful effect on QTc interval following single therapeutic or supratherapeutic doses of deferiprone.