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Related Experiment Videos

XEDS-mapping for explaining release patterns from single pellets.

Pernilla Nevsten1, Per Borgquist, Anders Axelsson

  • 1Department of Materials Chemistry/nCHREM, Lund University, P.O. Box 124, SE-221 00 Lund, Sweden. pernilla.nevsten@materialkemi.lth.se

International Journal of Pharmaceutics
|January 25, 2005
PubMed
Summary
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Pellet shape and surface defects significantly impact controlled-release pharmaceutical performance. Understanding these microscopic features is crucial for developing effective drug delivery systems.

Area of Science:

  • Pharmaceutical Sciences
  • Materials Science
  • Drug Delivery

Background:

  • Controlled-release (CR) pharmaceuticals are often formulated as polymer-coated pellets within capsules.
  • Understanding the relationship between pellet morphology and drug release is essential for optimizing CR formulations.

Purpose of the Study:

  • To investigate how pellet shape and surface structure influence the release profiles of CR pharmaceuticals.
  • To correlate microscopic pellet features with drug release rates and mechanisms.

Main Methods:

  • Scanning electron microscopy (SEM) and X-ray energy-dispersive spectrometry (XEDS) were used to analyze pellet surface structure before and after drug release.
  • Pellets were classified into spherical, dumbbell-shaped, and twin-pellet categories based on their morphology.

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  • Drug release profiles were monitored over time.

    • Main Results:

    • Surface defects, termed "open-window-defects," were identified as a cause of burst release across all pellet shapes.
    • Dumbbell-shaped pellets exhibited broader intermediate release rates due to thinner polymer films in neck regions.
    • Twin and dumbbell-shaped pellets showed more surface defects, leading to higher release rates compared to spherical pellets.
    • High release rates correlated with polymer film ruptures, while slow release rates showed only small cracks.

    Conclusions:

    • Pellet shape and surface integrity are critical determinants of controlled-release drug performance.
    • Microscopic analysis provides valuable insights for predicting and controlling drug release kinetics.
    • This knowledge is vital for the design of next-generation CR formulations and accurate mathematical modeling.