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Lipid membrane with low proton permeability.

Débora Nakai Biloti1, Maria Helena Andrade Santana, Francisco Benedito Teixeira Pessine

  • 1Department of Physical Chemistry, Institute of Chemistry, State University of Campinas (UNICAMP), Cx Postal 6154, 13084-971 Campinas, SP, Brazil.

Biochimica Et Biophysica Acta
|March 28, 2003
PubMed
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This study developed liposomes with low proton permeability, crucial for maintaining drug gradients. These advanced liposomes ensure stable intravesicular pH for effective drug delivery applications.

Area of Science:

  • Pharmaceutical Sciences
  • Biophysical Chemistry
  • Drug Delivery Systems

Background:

  • Liposomes are widely used drug delivery vehicles.
  • Maintaining a stable pH gradient across liposomal membranes is critical for certain drug formulations, such as those requiring encapsulation of weakly basic drugs.

Purpose of the Study:

  • To produce and characterize a liposomal formulation with demonstrably low proton permeability.
  • To confirm the ability of these liposomes to maintain a transmembranic pH gradient.

Main Methods:

  • Liposomes were formulated using specific lipids (DSPC, DSPE-PEG, DSPG, cholesterol) to achieve low internal pH.
  • Proton permeability was assessed using fluorescence quenching of 9-aminoacridine (9AA).
  • Carmofur (CPT-11) encapsulation was used to monitor intravesicular acidification over time.

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Main Results:

  • Physicochemical characterization confirmed the low proton permeability of the liposomal membrane.
  • The 9AA fluorescence quenching assay indicated minimal proton leakage.
  • CPT-11 encapsulation studies demonstrated the liposomes' capacity to sustain a transmembranic proton gradient.

Conclusions:

  • The developed liposomal formulation exhibits significantly low proton permeability.
  • This formulation is capable of maintaining a stable internal pH, making it suitable for applications requiring pH gradients, such as targeted drug delivery.