Fabrication and characterization of rutin-loaded liquid crystalline nanoparticles with in vitro anti-inflammatory and antitumor activities

Abstract

ABSTRACT A rutin-loaded liquid crystalline nanoparticle (R-LCNP) formulation was developed using glyceryl monooleate and Poloxamer 407 by high-pressure homogenization to improve the solubility and biological performance of rutin. The optimized R-LCNP-2 dispersion showed a mean particle size of 176.1 ± 4.5 nm, a polydispersity index (PDI) of 0.211 ± 0.013, and a moderately negative zeta potential of –20.4 ± 1.1 mV, consistent with steric-electrostatic stabilization. The encapsulation efficiency and drug loading were 98.1 ± 1.5% and 2.45 ± 0.04%, respectively, while FTIR, XRD, and DSC analyses indicated molecular dispersion of rutin within the lipid matrix. The formulation showed biphasic diffusion-controlled release and suppressed nitric oxide, TNF-α, and IL-6 more effectively than free rutin in an in vitro LPS-stimulated RAW 264.7 model. R-LCNP-2 also reduced the IC50 values in MCF-7, HeLa, and A549 cells by 3.8–4.5 fold relative to free rutin. These findings support LCNP-based encapsulation as a promising strategy to broaden the functional performance of rutin and justify subsequent in vivo pharmacokinetic and efficacy studies.