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Bioavailability Enhancement: Drug Permeability Enhancement01:27

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Body:After oral administration, poor permeability often limits the rate at which drugs are absorbed through the intestinal epithelium. Enhancing drug permeability is crucial for effective therapy, and several strategies have been developed to overcome this challenge.One effective strategy involves the use of lipid-based formulations. These formulations enhance dissolution and solubility, targeting physiological mechanisms to increase drug absorption. This includes stimulating bile salt...
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Lipoate-AmB-oleate-chol nanoparticles: An approach to decrease cytotoxic effects.

Victoria Leonhard1, Dante M Beltramo1, Laura R Comini1

  • 1Centro de Excelencia en Productos y Procesos de Córdoba, Ceprocor, Argentina; Consejo Nacional de Investigaciones Científicas y Técnicas, Conicet, Argentina.

Journal of Pharmaceutical Sciences
|September 22, 2025
PubMed
Summary
This summary is machine-generated.

Researchers developed novel nanoparticles by combining lipoic acid with the antifungal drug amphotericin B (AmB). These stable Lipoate-AmB nanoparticles show potent antifungal activity, with a new formulation reducing drug toxicity.

Keywords:
Amphotericin BCholesterolDrug-deliveryLipoic acidOleic acid micellesPhysicochemical characterization

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Area of Science:

  • Nanotechnology
  • Pharmaceutical Sciences
  • Mycology

Background:

  • Amphotericin B (AmB) is a potent antifungal drug with limited solubility and significant toxicity.
  • Lipoic acid can self-assemble into stable nanostructures in aqueous solutions.
  • Developing effective drug delivery systems is crucial for improving AmB's therapeutic index.

Purpose of the Study:

  • To characterize nanoparticles formed from lipoic acid and amphotericin B.
  • To evaluate the antifungal activity and stability of these Lipoate-AmB nanostructures.
  • To develop a less toxic formulation of AmB using cholesterol and sodium oleate.

Main Methods:

  • Spontaneous self-assembly of sodium lipoate nanostructures in aqueous media.
  • Incorporation of amphotericin B into lipoate nanostructures.
  • Formation and characterization of a quaternary complex including cholesterol and sodium oleate nanoparticles.
  • Assessment of biological activity and stability of the developed formulations.

Main Results:

  • Formation of stable Lipoate-AmB nanoparticles (25-60 nm) with a negative surface charge.
  • Lipoate-AmB complex demonstrated biological activity comparable to commercial formulations.
  • A quaternary complex (Lipoate-AmB-Oleate-Chol, ~100 nm) was formed, retaining antifungal activity with reduced toxicity.

Conclusions:

  • Lipoic acid can effectively form stable nanostructures with amphotericin B.
  • The developed Lipoate-AmB nanoparticles offer a promising alternative for antifungal therapy.
  • The quaternary complex represents a significant advancement in reducing AmB-associated side effects.