A slow cooling rate of indomethacin melt spatially confined in microcontainers increases the physical stability of the amorphous drug without influencing its biorelevant dissolution behaviour

Drug Delivery and Translational Research
Line Hagner NielsenThomas Rades

Abstract

Amorphous indomethacin was prepared by melting the γ-form of indomethacin, spatially confined within microcontainers (inner diameter of 223 μm), followed by cooling of the melt at a rate of 14, 23 or 36 K/min. The physical stability of the amorphous indomethacin within microcontainers was investigated using Raman microscopy. Furthermore, the dissolution behaviour of confined amorphous indomethacin was evaluated in biorelevant intestinal media at pH 6.5. After 30 days of storage, 10.3 ± 1.2 % of the amorphous indomethacin cooled at 14 K/min and confined within microcontainers was found to be crystalline. When the melt of indomethacin was cooled at 23 or 36 K/min, 20.7 ± 1.5 and 31.0 ± 2.6 % of the indomethacin were found to be crystalline after storage for 30 days. Scanning electron microscopy showed a smooth surface of amorphous indomethacin within the microcontainers when cooling the melt at 14 K/min, whereas cracks and an uneven surface were observed when cooling at rates of 23 and 36 K/min. The uneven surface is hypothesised to be the main reason for the lower physical stability, as the cracks could act as nucleation sites for crystal growth. The rate of cooling was not seen to have any effect on the dissolution of amorphous...Continue Reading

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Citations

Apr 2, 2016·International Journal of Pharmaceutics·Line Hagner NielsenAnja Boisen
Jul 6, 2018·Lab on a Chip·Line Hagner NielsenAnja Boisen
Apr 24, 2020·Advanced Healthcare Materials·Stine Egebro BirkAnja Boisen
May 31, 2021·Advanced Drug Delivery Reviews·Zhi LuoJean-Christophe Leroux
Jun 10, 2019·ACS Biomaterials Science & Engineering·Chiara MazzoniAnja Boisen

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European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V
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