Preparation and evaluation of licochalcone A - integrated casein-pectin nanodelivery system: Insights into its...

Licochalcone A (LCA) has many pHysiological functions, but its wide application is limited due to its low solubility and bioavailability. In this study, LCA-loaded casein-pectin nanoparticles (LCA-CS-P) were prepared using a pH-driven method to improve the release mechanism, and oral bioavailability of LCA. The results showed that the particle size, ζ-potential, polymer dispersity index, encapsulation efficiency and loading capacity of LCA-CS-P were 228 ± 3.56 nm, -32.5 ± 0.62 mV, 0.23 ± 0.02, 88.6 ± 1.12 %, and 22.5 ± 0.92 % respectively. Gastrointestinal digestion dynamically modulates the hydrogen bonding, electrostatic, and hydrophobic interactions within nanoparticles. This pH-responsive interaction reconfiguration governs their gastric stability, intestinal release, and increased bioavailability (2.47-fold AUC increase vs. free LCA). In addition, LCA-CS-P not only significantly increased the content of LCA in various tissues, but also had gastric targeting. Therefore, LCA-CS-P nanoparticles are a viable strategy to improve the oral bioavailability of LCA and other active ingredients.