Development of galangin-loaded nano-sized polyelectrolyte liposome: Optimization and characterization

Abstract

Galangin is a natural flavonol with high antioxidant properties and has a wide range characteristics of biological activity spectrum. Galangin has low solubility, permeability, and bioavailability, limiting its therapeutic use like many flavonoids. In this study, nano-sized polyelectrolyte liposomes were developed and characterized to overcome the properties that limit the use of galangin. The various parameters (phospholipid/solvent ratio, cholesterol/solvent ratio, time and galangin/solvent ratio) were optimized with a response surface methodology-central composite design to develop liposomes with maximum encapsulation efficiency using the thin-film hydration method. An optimum liposome formulation was developed with 93.77 +/- 0.05% encapsulation efficiency, a spherical large unilamellar vesicle with a size of 485.5 +/- 128.41 nm, and a zeta potential of - 48 +/- 7 mV. The optimum liposome formulation was coated with polyelectrolyte biopolymer chitosan (CH) and gum arabic (GUA) using the layer-by-layer deposition method to improve its stability and drug release profile. The CH-liposome has a size of 208.05 +/- 73.04 nm and a zeta potential of + 40 +/- 5 mV. The GUA-CH-liposome has a size of 266.60 +/- 8.49 nm and a zeta potential of - 6 mV. Fourier transform infrared spectroscopy analysis showed that galangin was encapsulated without disturbing the liposome structure and the polyelectrolyte coated the surface with electrostatic interaction. At the end of the in vitro release study, GUA-CH-liposome released 23.84% of galangin. Regarding stability, drug loading capacity of GUA-CH-liposome, which was 93.77 +/- 0.05% on day 0, changed to 92.72 +/- 0.51% at + 4 degrees C, 93.09 +/- 0.01% at room temperature and 93.15 +/- 0.01% at - 24 degrees C on day 28.