Structural properties induced by the composition of biocompatible phospholipid-based microemulsion and amphotericin B

Cristina Maria Franzini1, Kelly Christina Pestana, Eduardo Ferreira Molina

  • 1Universidade Estadual Paulista, UNESP, Faculdade de Ciências Farmacêuticas, Programa de Pós-graduação em Ciências Farmacêuticas, Rodovia Araraquara-Jaú km 01, 14801-902, Araraquara, SP, Brazil.

Insights

Anionic microemulsions (MEs) effectively carry amphotericin B, with droplet size influenced by surfactant and oil content. Formulation composition dictates drug loading and system structure for optimized drug delivery.

Area of Science:

  • Colloid and Surface Chemistry
  • Pharmaceutical Nanotechnology
  • Drug Delivery Systems

Background:

  • Anionic microemulsions (MEs) are explored as potential nanocarriers for drug delivery.
  • The interaction between drug molecules and ME components influences carrier performance.
  • Amphotericin B is an antifungal agent often requiring effective delivery systems.

Purpose of the Study:

  • To investigate anionic microemulsions (MEs) formulated with soya phosphatidylcholine, Tween-20, and sodium oleate as drug carriers for amphotericin B.
  • To characterize the structural and physicochemical properties of these MEs.
  • To understand the influence of ME composition on amphotericin B incorporation and system behavior.

Main Methods:

  • Microemulsion formulation using soya phosphatidylcholine, Tween-20, sodium oleate, and cholesterol.
  • Characterization techniques including photon correlation spectroscopy, rheological behavior analysis, and polarized light microscopy.
  • Investigation of amphotericin B incorporation and its dependence on microemulsion composition.

Main Results:

  • Droplet diameters increased with amphotericin B incorporation.
  • Surfactant concentration stabilized droplets, while increased oil phase led to larger droplet diameters.
  • Amphotericin B incorporation increased with oil phase and surfactant concentration, reaching a plateau.
  • Rheological analysis indicated pseudoplastic behavior with slight thixotropy.
  • Increased oil-to-surfactant ratio induced lamellar arrangements in microemulsions.

Conclusions:

  • Anionic microemulsions are viable carriers for amphotericin B, with tunable properties based on formulation.
  • The pseudo-phase model effectively describes amphotericin B distribution within the microemulsion system.
  • Formulation composition significantly impacts microemulsion structure and drug loading capacity.

Related Concept Videos

Antifungal Agents01:15

Antifungal Agents

Amphotericin B is a broad-spectrum antifungal agent that exploits structural differences between fungal and mammalian cell membranes. Its amphipathic structure—featuring a hydrophobic polyene-lactone ring and a hydrophilic region containing mycosamine and carboxylic acid groups—enables selective binding to ergosterol, a sterol predominantly found in fungal plasma membranes. This selective interaction underlies the drug’s antifungal activity, although weak binding to cholesterol contributes to...
Micelles01:30

Micelles

Micelle formation is an intricate process that hinges on the properties of amphiphilic or amphipathic molecules and the conditions of the system in which they are found. Amphiphilic molecules, which have both hydrophilic (water-attracting) and hydrophobic (water-repelling) parts, play a critical role in this process.In aqueous environments, these molecules arrange themselves such that their hydrophilic heads are turned towards the water phase, while their hydrophobic tails are oriented away...
Asymmetric Lipid Bilayer01:35

Asymmetric Lipid Bilayer

Biological membranes show uneven distribution of different types of lipids in the inner and outer layers, resulting in transverse asymmetric membranes. The treatment of the erythrocyte membrane with the enzyme phospholipase confirmed the asymmetric nature of the lipid bilayer. The enzyme hydrolyzes lipids into fatty acids and hydrophilic groups. The phospholipase acts only on the outer layer of the membrane, while the inner layer remains intact. The phospholipase treatment resulted in 80%...
Biosynthesis of Lipids01:29

Biosynthesis of Lipids

Microbial membranes exhibit remarkable diversity in lipid composition, reflecting evolutionary adaptations to various environmental conditions. The three domains of life—Bacteria, Archaea, and Eukarya—synthesize membrane lipids through distinct biosynthetic pathways, leading to fundamental structural differences that impact membrane stability, function, and adaptability.Fatty Acid-Based Lipids in Bacteria and EukaryaBacteria and eukaryotes share a common fatty acid biosynthesis pathway, which...
Membrane Fluidity01:23

Membrane Fluidity

Cell membranes are composed of phospholipids, proteins, and carbohydrates loosely attached to one another through chemical interactions. Molecules are generally able to move about in the plane of the membrane, giving the membrane its flexible nature called fluidity. Two other features of the membrane contribute to membrane fluidity: the chemical structure of the phospholipids and the presence of cholesterol in the membrane.
Membrane Fluidity01:26

Membrane Fluidity

Membrane fluidity is explained by the fluid mosaic model of the cell membrane, which describes the plasma membrane structure as a mosaic of components—including phospholipids, cholesterol, proteins, and carbohydrates—that gives the membrane a fluid character.
Mosaic nature of the membrane
The mosaic characteristic of the membrane helps the plasma membrane remain fluid. The integral proteins and lipids exist as separate but loosely-attached molecules in the membrane. The membrane is a relatively...