Title : Formulation of xanthohumol-loaded polylactic acid nanoparticles
Abstract:
Xanthohumol is a natural compound with promising antioxidant, anti-inflammatory and anticancer properties, but its clinical application is limited due to poor water solubility and low bioavailability. Incorporating xanthohumol into polymer nanoparticles can enhance its stability, solubility, and may provide a controlled-release profile. This strategy aims to improve the drug therapeutic potential by facilitating targeted delivery and prolonged drug release.
Aim: The aim of this study was to develop polylactic acid (PLA) nanoparticles using an emulsification method with solvent evaporation and to evaluate their potential as drug delivery systems for Xanthohumol.
Materials and methods: A 32 full factorial design was applied in order to estimate the effect of the independent variables (concentration of the emulsifier Tween 80 and the stirring rate) over the dependent variables (average particle size, zeta potential and production yield). The conducted analysis was used to define optimal production parameters. The independent variables were varied at three levels (+1, 0, -1), as the concentration of Tween 80 was 0.5%, 1.0% and 1.5% and the stirring rate: 15 000 rpm, 20 000 rpm and 25 000 rpm. Based on the obtained optimal model of PLA nanostructures, two batches of Xanthohumol-loaded nanoparticles were synthesized at different polymer to drug ratios (1:1 and 2:1). The formulated nanostructures were characterized in terms of particle size, particle size distribution and zeta potential using dynamic and electrophoretic light scattering. Nanoparticles shape and surface morphology were observed using scanning electron microscopy.
Results: The obtained structures had average particle size in the range from 240 nm to 280 nm, zeta potential of -30 mV and production yield between 75% and 87%. Drug loading varied between 25% and 45% and the drug encapsulation efficacy was in the range from 68% to 84%. Delayed in vitro drug release was observed for both batches, being more prominent in the batch prepared at polymer to drug ratio 1:2. The formulated nanoparticles demonstrate significant potential as a promising drug delivery system for the effective delivery of xanthohumol.
Acknowledgments: This research was funded by the European Union-NextGenerationEU, through the National Recovery and Resilience Plan of the Republic of Bulgaria project number BG-RRP-2.004-0007-C01.
