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Related Experiment Videos

Interactions of griseofulvin with cyclodextrins in solid binary systems

M D Veiga1, P J Díaz, F Ahsan

  • 1Departamento de Farmacia y Tecnología Farmacéutica, Facultad de Farmacia, Universidad Complutense de Madrid, 28040-Madrid, Spain.

Journal of Pharmaceutical Sciences
|July 2, 1998
PubMed
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Griseofulvin solubility and dissolution improved with cyclodextrins. While solid-state interactions were minimal, an in situ inclusion complex formed in aqueous media, enhancing drug performance.

Area of Science:

  • Pharmaceutical Sciences
  • Physical Chemistry

Background:

  • Griseofulvin is an antifungal agent with poor aqueous solubility.
  • Cyclodextrins (CDs) are known to enhance the solubility and bioavailability of poorly soluble drugs.

Purpose of the Study:

  • To investigate the solid-state and aqueous interactions between griseofulvin and two cyclodextrin derivatives: beta-cyclodextrin (β-CD) and 2-hydroxypropyl beta-cyclodextrin (HPβ-CD).
  • To evaluate the impact of these interactions on griseofulvin's solubility and dissolution rate.

Main Methods:

  • Preparation of physical mixtures and kneaded systems of griseofulvin with β-CD and HPβ-CD at 1:1 and 1:2 mol/mol ratios.
  • Characterization using Scanning Electron Microscopy (SEM), Hot-Stage Microscopy (HSM), Differential Scanning Calorimetry (DSC), Thermogravimetry (TG), and X-ray Powder Diffractometry (XRPD).

Related Experiment Videos

  • Assessment of griseofulvin solubility and dissolution profiles.

    • Main Results:

    • Griseofulvin solubility increased with increasing cyclodextrin concentration.
    • HSM indicated dissolution of HPβ-CD in melted griseofulvin, but no interaction with β-CD.
    • DSC and XRPD suggested the absence of a stable solid-state inclusion complex between griseofulvin and either cyclodextrin.
    • All binary systems demonstrated improved griseofulvin dissolution rates.

    Conclusions:

    • Solid-state complexation between griseofulvin and the studied cyclodextrins was not evident.
    • An "in situ" drug/cyclodextrin inclusion complex likely formed in the aqueous dissolution medium, leading to enhanced griseofulvin solubility and dissolution.
    • HPβ-CD showed potential for improving griseofulvin's dissolution characteristics.