Glucosylated liposomes as drug delivery systems of usnic acid to address bacterial infections

Colloids Surf B Biointerfaces. 2019 Sep 1:181:632-638. doi: 10.1016/j.colsurfb.2019.05.056. Epub 2019 Jun 4.

Abstract

Because of the increased incidence of infections caused by resistant pathogens, due to the intensive use of antibiotics, there is an urgent need to develop new therapeutic strategies against bacteria, possibly based on non conventional drugs. (+)-Usnic acid is a natural compound that exerts a potent antibacterial activity, however its clinical application is hampered by its scarce solubility in water. Usnic acid was included, by both passive and active loading techniques, in liposomes containing structurally related glucosylated amphiphiles. Liposome formulations were characterized from the physicochemical point of view and their activity against biofilm associated Staphylococcus epidermidis was also evaluated. The inclusion of usnic acid in glucosylated cationic liposomes promotes its penetration in biofilm matrix with a consequent increase of its antimicrobial activity. The effect of both cationic charge and sugar residue seems to be synergistic.

Keywords: (+)-Usnic acid; Glycosylation; Liposomes; Positive charge; Staphylococcus epidermidis biofilm.

MeSH terms

  • Anti-Bacterial Agents / chemistry
  • Anti-Bacterial Agents / pharmacology*
  • Bacterial Infections / drug therapy*
  • Benzofurans / chemistry
  • Benzofurans / pharmacology*
  • Biofilms / drug effects
  • Drug Delivery Systems*
  • Glycosylation
  • Liposomes / chemical synthesis
  • Liposomes / chemistry
  • Microbial Sensitivity Tests
  • Molecular Structure
  • Particle Size
  • Staphylococcus epidermidis / drug effects*
  • Surface Properties

Substances

  • Anti-Bacterial Agents
  • Benzofurans
  • Liposomes
  • usnic acid