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Related Experiment Videos

Microcrystallization of indomethacin using a pH-shift method.

Sung-Tae Kim1, Jai-Hyun Kwon, Jae-Jeong Lee

  • 1Graduate School of Life Sciences and Biotechnology, Korea University, 5-1 Anam-Dong, Sungbuk-Ku, Seoul 136-701, South Korea.

International Journal of Pharmaceutics
|September 5, 2003
PubMed
Summary

This study created indomethacin microcrystals using a pH-shift method. These microcrystals showed improved dissolution and biological activity for potential anti-inflammatory and anti-cancer applications.

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Area of Science:

  • Pharmaceutical Sciences
  • Materials Science

Background:

  • Indomethacin, a nonsteroidal anti-inflammatory drug (NSAID), is widely used for pain and inflammation.
  • Improving the bioavailability and efficacy of NSAIDs is crucial for enhanced therapeutic outcomes.
  • Microcrystallization offers a promising approach to modify drug properties.

Purpose of the Study:

  • To develop a microcrystallization process for indomethacin using a pH-shift method.
  • To characterize the physicochemical properties of the resulting indomethacin microcrystals.
  • To evaluate the dissolution rate and biological activity of the microcrystals.

Main Methods:

  • pH-shift method in aqueous solution for indomethacin microcrystallization.
  • Physicochemical characterization using X-ray diffraction (XRD), differential scanning calorimetry (DSC), and Fourier transform infrared spectroscopy (FT-IR).

Related Experiment Videos

  • Morphological analysis via phase contrast microscopy and scanning electron microscopy (SEM).
  • Dissolution rate testing and in vitro biological activity assessment (colon cancer cell proliferation inhibition).

    • Main Results:

    • Microcrystallization yielded plate-like indomethacin microcrystals with uniform size (10.4±0.4 µm).
    • Physicochemical properties were comparable to standard indomethacin, with minor reductions in XRD peak height and melting temperature.
    • Indomethacin microcrystals exhibited a 2.2-fold higher initial dissolution rate.
    • Biological activity against HT-29 colon cancer cells was approximately 20% higher.

    Conclusions:

    • The pH-shift microcrystallization method effectively produced indomethacin microcrystals with desirable characteristics.
    • Enhanced dissolution and biological activity suggest potential therapeutic advantages for indomethacin microcrystals.
    • This approach could be valuable for improving the delivery and efficacy of indomethacin and other NSAIDs.