Preparation of alginate beads containing a prodrug of diethylenetriaminepentaacetic acid.

Yu-Tsai Yang, Anthony J Di Pasqua, Weiling He, Tsuimin Tsai, Katsuhiko Sueda, Yong Zhang, Michael Jay

Index: Carbohydr. Polym. 92(2) , 1915-20, (2013)

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Abstract

A penta-ethyl ester prodrug of the radionuclide decorporation agent diethylenetriaminepentaacetic acid (DTPA), which exists as an oily liquid, was encapsulated in alginate beads by the ionotropic gelation method. An optimal formulation was found by varying initial concentrations of DTPA penta-ethyl ester, alginate polymer, Tween 80 surfactant and calcium chloride. All prepared alginate beads were ~1.6mm in diameter, and the optimal formulation had loading and encapsulation efficiencies of 91.0±1.1 and 72.6±2.2%, respectively, and only 3.2±0.8% water absorption after storage at room temperature in ~80% relative humidity. Moreover, Fourier transform infrared spectroscopy showed that DTPA penta-ethyl ester did not react with excipients during formation of the DTPA penta-ethyl ester-containing alginate beads. Release of prodrug from alginate beads was via anomalous transport, and its stability enhanced by encapsulation. Collectively, these data suggest that this solid dosage form may be suitable for oral administration after radionuclide contamination.Copyright © 2012 Elsevier Ltd. All rights reserved.