Structural Changes in Liposomal Vesicles in Association with Sodium Taurodeoxycholate

AAPS PharmSciTech. 2023 Apr 3;24(4):95. doi: 10.1208/s12249-023-02550-7.

Abstract

Liposomes composed of soy lecithin (SL) have been studied widely for drug delivery applications. The stability and elasticity of liposomal vesicles are improved by incorporating additives, including edge activators. In this study, we report the effect of sodium taurodeoxycholate (STDC, a bile salt) upon the microstructural characteristics of SL vesicles. Liposomes, prepared by the thin film hydration method, were characterized by dynamic light scattering (DLS), small-angle neutron scattering (SANS), electron microscopy, and rheological techniques. We noticed a reduction in the size of vesicles with the incremental addition of STDC. Initial changes in the size of spherical vesicles were ascribed to the edge-activating action of STDC (0.05 to 0.17 µM). At higher concentrations (0.23 to 0.27 µM), these vesicles transformed into cylindrical structures. Morphological transitions at higher STDC concentrations would have occurred due to its hydrophobic interaction with SL molecules in the bilayer. This was ascertained from nuclear magnetic resonance observations. Whereas shape transitions underscored the deformability of vesicles in the presence of STDC, the consistency of bilayer thickness ruled out any dissociative effect. It was interesting to notice that SL-STDC mixed structures could survive high thermal stress, electrolyte addition, and dilution.

Keywords: bile salt; edge activator; elasticity; liposomes; mixed vesicles; soy lecithin.

MeSH terms

  • Drug Delivery Systems
  • Liposomes* / chemistry
  • Micelles
  • Polymers
  • Scattering, Small Angle
  • Taurodeoxycholic Acid*

Substances

  • Liposomes
  • Taurodeoxycholic Acid
  • Micelles
  • Polymers