Introduction: Flavonoids such as rutin (R) and quercetin (Q) are natural polyphenolic compounds with significant pharmacological activities and a key role in disease prevention. They exhibit strong anti-inflammatory, antioxidant, and vasoprotective properties. However, their poor aqueous solubility markedly limits their bioavailability and therapeutic efficacy [1]. Herein, Chitosan-based nanoparticles (CS-NPs) encapsulating R and Q were developed using electrofluid dynamic (EFD) and ionotropic gelation (IG) techniques, resulting in enhanced controlled release profiles suitable for mitigating vascular inflammation.
Method: R and Q were preliminarily subjected to physicochemical characterization, including phase solubility studies, melting point determination, and FTIR spectroscopy. CS-NPs singularly loaded with R or Q were optimized adapting the preparation methods reported in previous studies [2,3], in order to improve drug loading and stability. Different formulations were characterized in terms of particle size, polydispersity index (PDI), zeta potential (ZP), and morphology (SEM, TEM). Encapsulation efficiency (EE %) was determined and in vitro release kinetics were evaluated and fitted using mathematical models.
Results: The CS-NPs exhibited a mean diameter of 200–350 nm, depending on the preparation method and processing parameters. The PDI was approximately 0.22, indicating good formulation homogeneity, while the ZP was around +28 mV, reflecting the characteristic positive surface charge of chitosan and ensuring colloidal stability. All samples showed high encapsulation efficiency (EE ≈ 95%). R- and Q-loaded CS-NPs prepared by EFD showed greater drug release compared to those obtained via IG. In vitro release profiles were best fitted by the Korsmeyer-Peppas model, suggesting a diffusion-controlled mechanism, involving both R and Q diffusion and polymer relaxation.
Conclusion: R‑ and Q‑loaded CS‑NPs showed favorable physicochemical properties, high entrapment efficiency, and controlled, diffusion‑driven release. In vitro studies in inflammatory cell models are ongoing to assess their anti‑inflammatory activity and potential as bioavailable nanocarriers for preventing and targeting vascular inflammation.
