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Membrane fluidization by animycotic bifonazole

G Albertini1, G Bossi, B Dubini

  • 1Dipartimento di Scienze dei Materiali e della Terra, University, Ancona Italy.

Physiological Chemistry and Physics and Medical NMR
|January 1, 1995
PubMed
Summary
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Bifonazole drug increases fluidity and permeability of dipalmitoyl phosphatidylcholine (DPPC) liposomes. This antifungal agent alters lipid matrix properties, affecting membrane structure and ion transport.

Area of Science:

  • Lipid bilayer biophysics
  • Antifungal drug interactions
  • Membrane biophysics

Background:

  • Dipalmitoyl phosphatidylcholine (DPPC) liposomes are crucial in drug delivery.
  • Understanding drug-lipid interactions is vital for effective formulations.
  • Bifonazole is an antifungal agent with potential membrane-active properties.

Purpose of the Study:

  • To investigate the thermodynamic and structural effects of bifonazole on DPPC liposomes.
  • To evaluate the impact of bifonazole on liposome fluidity, permeability, and phase transitions.
  • To characterize the structural organization of bifonazole-doped DPPC liposomes.

Main Methods:

  • Differential Scanning Calorimetry (DSC) for thermodynamic analysis.
  • Electron Spin Resonance (ESR) spectroscopy for fluidity and permeability studies.

Related Experiment Videos

  • Nuclear Magnetic Resonance (NMR) and X-ray diffraction for structural characterization.
  • Transmission Electron Microscopy (TEM) for visualizing liposome morphology.

    • Main Results:

    • Bifonazole incorporation decreased the cooperativity of the gel to liquid crystalline phase transition, indicating increased lipid matrix fluidity.
    • ESR studies showed increased membrane permeability to ascorbate ions upon bifonazole addition.
    • 13C NMR revealed that the bifonazole molecule is highly immobilized within the DPPC matrix.
    • X-ray diffraction and TEM confirmed a lamellar, unidimensional phase at room temperature, with uniform particles and pits, and significant hysteresis in phase formation.

    Conclusions:

    • Bifonazole significantly alters the physical properties of DPPC liposomes, enhancing fluidity and permeability.
    • The drug's immobilization suggests specific interactions within the lipid bilayer.
    • The observed structural changes and hysteresis indicate complex phase behavior influenced by bifonazole.