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Physicochemical characterization and dissolution properties of nimesulide-cyclodextrin binary systems.

Buchi N Nalluri1, K P R Chowdary, K V R Murthy

  • 1Department of Pharmaceutical Sciences, Andhra University, Visakhapatnam, India. buchi999@yahoo.com

AAPS Pharmscitech
|August 15, 2003
PubMed
Summary
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This study enhanced nimesulide dissolution by complexing it with cyclodextrins (CDs). Nimesulide-cyclodextrin systems showed improved physicochemical properties and dissolution rates compared to pure nimesulide.

Area of Science:

  • Pharmaceutical Sciences
  • Physical Chemistry
  • Materials Science

Background:

  • Nimesulide is a non-steroidal anti-inflammatory drug (NSAID) with poor aqueous solubility, limiting its therapeutic efficacy.
  • Cyclodextrins (CDs) are cyclic oligosaccharides with a hydrophobic cavity and hydrophilic exterior, widely used to improve the solubility and bioavailability of poorly soluble drugs.

Purpose of the Study:

  • To characterize the physicochemical properties of nimesulide-cyclodextrin (N-CD) binary systems.
  • To investigate the formation of inclusion complexes between nimesulide and alpha-, beta-, and gamma-cyclodextrins.
  • To enhance the dissolution properties of nimesulide through complexation with CDs.

Main Methods:

  • Solution studies: Phase solubility analysis, mass spectrometry, and 1H nuclear magnetic resonance (1H-NMR) spectroscopy.

Related Experiment Videos

  • Solid-state studies: Differential scanning calorimetry (DSC), powder X-ray diffractometry (X-RD), and scanning electron microscopy (SEM).
  • In vitro dissolution studies were conducted to assess the impact of complexation on drug release.

    • Main Results:

    • Solution studies confirmed 1:1 molar complexation between nimesulide and all tested cyclodextrins.
    • Solid-state characterization indicated a 1:2 molar inclusion complex of nimesulide with beta-cyclodextrin.
    • Nimesulide-cyclodextrin binary systems exhibited significantly superior dissolution properties compared to pure nimesulide.

    Conclusions:

    • Complexation with alpha-, beta-, and gamma-cyclodextrins effectively improves the physicochemical properties of nimesulide.
    • The formation of inclusion complexes, particularly with beta-cyclodextrin, enhances nimesulide's dissolution rate.
    • These findings suggest that cyclodextrin complexation is a viable strategy for improving nimesulide's pharmaceutical formulation.