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Related Experiment Videos

Melarsoprol-cyclodextrins inclusion complexes.

Stéphane Gibaud1, Siham Ben Zirar, Pierre Mutzenhardt

  • 1Laboratoire de Pharmacie Clinique, EA 3452, Faculté de Pharmacie, 5 Rue Albert Lebrun, 54000 Nancy, France. stephane.gibaud@pharma.uhp-nancy.fr

International Journal of Pharmaceutics
|October 29, 2005
PubMed
Summary
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Melarsoprol cyclodextrin complexes were developed to enhance drug tolerability and bioavailability. Complexation improved solubility and dissolution but did not alter the cytotoxic effects on leukemia cells.

Area of Science:

  • Pharmaceutical Sciences
  • Drug Delivery
  • Medicinal Chemistry

Background:

  • Melarsoprol is a water-insoluble drug used for trypanosomiasis with in vitro activity against leukemia cell lines.
  • The current non-aqueous formulation (Arsobal) exhibits poor tolerability.
  • Improving melarsoprol's bioavailability and tolerability is crucial for its therapeutic application.

Purpose of the Study:

  • To develop melarsoprol-cyclodextrin complexes to enhance drug tolerability and bioavailability.
  • To investigate the complexation behavior and stoichiometry of melarsoprol with various cyclodextrins.
  • To evaluate the impact of complexation on melarsoprol's solubility, dissolution rate, and cytotoxic activity.

Main Methods:

  • Phase-solubility analysis to determine complex formation and stoichiometry.

Related Experiment Videos

  • UV spectrophotometry (Job's plot) to confirm 1:1 inclusion complex stoichiometry.
  • 1H-NMR and ROESY experiments to elucidate the inclusion complex structure.
  • Evaluation of solubility enhancement, stability constants, and dissolution rates.
  • Assessment of cytotoxic properties on K562 and U937 human leukemia cell lines.

    • Main Results:

    • Phase-solubility studies indicated 1:1 inclusion complex formation with beta-cyclodextrin (betaCD), randomly methylated beta-cyclodextrin (RAMEbetaCD), and hydroxypropyl-beta-cyclodextrin (HPbetaCD).
    • Solubility enhancement factors reached approximately 7.2x10^3 with betaCD derivatives.
    • High apparent stability constants (K(1:1)) were determined for RAMEbetaCD (57,143 M⁻¹) and HPbetaCD (50,761 M⁻¹).
    • NMR data confirmed melarsoprol inclusion into the cyclodextrin torus.
    • RAMEbetaCD significantly improved melarsoprol's hydrolysis and dissolution rate.
    • Cytotoxicity against leukemia cell lines remained unchanged post-complexation.

    Conclusions:

    • Melarsoprol-cyclodextrin complexation effectively enhances solubility and dissolution, potentially improving bioavailability.
    • RAMEbetaCD and HPbetaCD are suitable complexing agents for melarsoprol.
    • The observed improvement in physicochemical properties did not affect the drug's inherent cytotoxic activity against leukemia cells.