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Related Experiment Videos

Interactions between lonidamine and beta- or hydroxypropyl-beta-cyclodextrin

G F Palmieri1, P Wehrlé, S Martelli

  • 1Dipartimento di Scienze Chimiche, Università di Camerino, Italy.

Drug Development and Industrial Pharmacy
|January 7, 1999
PubMed
Summary
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This study explored forming inclusion complexes of lonidamine with cyclodextrins to enhance water solubility. Spray-drying proved most effective for creating these complexes, improving drug dissolution.

Area of Science:

  • Pharmaceutical Sciences
  • Drug Delivery Systems
  • Physical Chemistry

Background:

  • Lonidamine is an anticancer agent with poor water solubility, limiting its therapeutic efficacy.
  • Cyclodextrins are known to form inclusion complexes with poorly soluble drugs, potentially improving their physicochemical properties.

Purpose of the Study:

  • To investigate the formation of inclusion complexes between lonidamine and beta-cyclodextrin or hydroxypropyl-beta-cyclodextrin.
  • To evaluate different complexation methods (spray-drying, kneading, solid dispersion) for optimizing lonidamine solubility.
  • To characterize the interaction between lonidamine and cyclodextrins and assess the dissolution profiles of the resulting complexes.

Main Methods:

  • Phase solubility diagrams were used to assess complexation potential.

Related Experiment Videos

  • Differential scanning calorimetry (DSC) and X-ray diffractometry (XRD) were employed for solid-state characterization.
  • Spray-drying, kneading, and solid dispersion techniques were applied for complex preparation.
  • Dissolution studies were conducted to evaluate the impact of complexation on lonidamine release.

    • Main Results:

    • Phase solubility studies indicated the feasibility of forming inclusion complexes.
    • DSC and XRD analyses revealed external interactions between lonidamine and cyclodextrins, suggesting complex formation.
    • Spray-drying was identified as a promising method for preparing lonidamine-cyclodextrin complexes.
    • The prepared complexes demonstrated improved dissolution profiles compared to pure lonidamine.

    Conclusions:

    • Inclusion complexation with beta-cyclodextrin and hydroxypropyl-beta-cyclodextrin can enhance lonidamine's water solubility and dissolution rate.
    • Spray-drying is an effective method for preparing these inclusion complexes.
    • Further optimization of molar ratios and preparation techniques may lead to improved therapeutic outcomes for lonidamine.