Aug 2026· International Journal of Biological Macromolecules· Vol 381, pp.
154179
· 0 citations· 25 references
Medicine
TL;DR
These findings establish gliadin-fucoidan macromolecular assembly as a pH-responsive and biologically functional oral nanoplatform for renal inflammation.
Abstract
Gliadin and fucoidan are biologically active macromolecules with complementary self-assembly, drug-binding, and anti-inflammatory properties. Here, gliadin/naringenin@fucoidan nanoparticles (NPs) were engineered through antisolvent precipitation followed by electrostatic self-assembly to improve the oral delivery and renoprotective activity of naringenin. Gliadin, a 35-40 kDa wheat protein, formed the hydrophobic drug-loaded core, whereas sulfated fucoidan formed a functional polysaccharide shell through electrostatic interactions and hydrogen bonding. The NPs exhibited spherical core-shell morphology, a transmission electron microscopy diameter of 100-110 nm, a hydrodynamic diameter of 108.3 nm, and a pH-dependent surface charge. Nuclear magnetic resonance, Fourier-transform infrared spectroscopy, and X-ray diffraction confirmed gliadin-naringenin molecular interactions, fucoidan surface deposition, and conversion of crystalline naringenin into an amorphous molecular dispersion. The optimized formulation achieved 41.11% encapsulation efficiency and a loading capacity of 30.83 μg/mL. Fucoidan coating restricted naringenin release to 13.95% at pH 2.0 but increased release to 77.15% at pH 7.0. In lipopolysaccharide (LPS)-injured HEK-293 cells, the core-shell NPs restored viability to 93.18%, reduced reactive oxygen species from 181.0 to 74.3, and limited early and late apoptosis to 4.35% and 4.58%, respectively. Cellular fluorescence intensity increased 7.7-fold relative to free naringenin. In septic acute kidney injury mice, oral treatment reduced blood urea nitrogen, creatinine, kidney injury molecule-1, and neutrophil gelatinase-associated lipocalin to 7.10 mmol/L, 25.05 μmol/L, 94.87 pg/mL, and 177.37 ng/mL, respectively. These findings establish gliadin-fucoidan macromolecular assembly as a pH-responsive and biologically functional oral nanoplatform for renal inflammation.
This study proposes a novel strategy to overcome the trade-off between high inhibitory activity against Advanced glycation end-products and processing stability of natural polyphenols by designing proanthocyanidin‑iron microspheres. These microspheres were fabricated via coordination-driven self-assembly of iron ions and proanthocyanidins, followed by coating with sodium alginate. Characterization using scanning electron microscopy, Raman spectroscopy, X-ray diffraction, X-ray photoelectron spectroscopy, Fourier transform infrared spectroscopy, and ultraviolet-visible spectroscopy revealed the structural characteristics and interfacial interactions of the microspheres. Molecular docking simulations verified a high-affinity interaction between proanthocyanidins and bovine serum albumin, with a binding free energy difference of 3.30 kcal/mol. In a biscuit model, the microspheres exhibited dose-dependent inhibition of fluorescent advanced glycation end-products(58.7%)at the highest tested concentration. This work establishes proanthocyanidin‑iron microspheres as a potential functional food ingredient with anti-glycation properties, providing a viable strategy for dietary intervention by controlling deleterious compounds in processed foods.
Dong Chen, Zhi-Yu Huang, Xing-Ru Wang et al.· Food Chemistry· 0 citations
Superparamagnetic iron oxide nanoparticles (SPIONs-Fe3O4) functionalized with l-cysteine (SPIONs-l-Cys) were evaluated as a biocompatible, magnetically responsive nanosystem in an Ehrlich solid tumor model. The formulation was obtained by chemical coprecipitation, and its complementary physicochemical characterization is provided in the Supporting Information and supported by our previous report on the same l-cysteine-functionalized magnetite system, including X-ray diffraction, FTIR, hydrodynamic size, polydispersity index, ζ-potential, surface thiol quantification by DTNB, magnetic measurements, and complementary in vitro data. The supplementary characterization supports the preservation of the magnetite crystalline structure after functionalization and confirms the presence of free thiol groups in an aqueous dispersion. In vitro cytotoxicity assays using human mononuclear cells and Ehrlich tumor cells indicated low toxicity under selected experimental conditions and biologically relevant redox-associated activities. In vivo evaluation demonstrated preserved hematological and biochemical parameters, the absence of overt systemic toxicity, and reduced tumor burden in groups treated with SPIONs-l-Cys under magnetic targeting conditions. These findings support the biological compatibility of SPIONs-l-Cys and indicate antitumor-associated effects under localized magnetic field conditions, while not establishing intratumoral accumulation, drug delivery, or a definitive mechanism of action.
E. B. da Silva, T. Britos, C. Chagas et al.· ACS Omega· 0 citations
Designing multifunctional nanocarriers that integrate controlled drug delivery, favorable protein interactions, and accelerated tissue repair remains a key challenge in nanomedicine. In this study, we have engineered a magnetically responsive, biocompatible Fe3O4@SiO2 nanoparticle functionalized with a bromocholine-based ionic liquid. This surface design enabled efficient encapsulation and sustained release of the hydrophobic anticancer drug quercetin over 72 h under physiological conditions. Given the critical role of plasma protein adsorption in determining nanomaterial fate, systematic interaction studies with human serum albumin (HSA) were investigated using spectroscopic analyses, molecular docking, and esterase-like activity assays. The results showed that the nanocarriers exhibited stable protein binding with minimal conformational perturbation and preserved enzymatic activity, indicating excellent biocompatibility. Further, in an in vivo wound healing model, topical application of quercetin-loaded nanocarriers at 500 ppm led to rapid wound closure, with significant wound reduction observed within 3 h. The magnetic core further offers potential for external guidance to wound sites. Overall, this bromocholine-functionalized platform combines tunable drug release, biointerfacial compatibility, and rapid healing efficacy, making it a promising candidate for advanced wound therapy.
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.
Escherichia coli-induced enteritis imposes a substantial economic burden on the global livestock industry. In the current context of reducing and restricting antibiotic use, there is an urgent need for novel therapeutic strategies. Based on traditional Chinese medicine compatibility, anemoside B4 (AB4) and oleanolic acid (OA) form nanoscale assemblies (AB4-OA NPs) through hydrogen bonds and van der Waals forces. Physicochemical characterization quantified the NPs as spherical particles with an average hydrodynamic diameter of 164.16 nm, a PDI of 0.280, zeta potential of −22.16 mV, and stable particle size for 28 days; the hemolysis ratio remained below 3.38% at concentrations up to 2 mg/mL, confirming favorable biosafety. In vitro assays confirmed that AB4-OA NPs outperformed AB4/OA physical mixtures in anti-inflammatory and antioxidant activity by restraining pro-inflammatory factors and activating antioxidant enzymes, verifying nanotechnology’s potency in boosting their bioactivity. In mice challenged intraperitoneally with E. coli, AB4-OA NPs elevated SOD, CAT, GSH-Px and lowered MDA; they inhibited the NF-κB pathway, activated the Nrf2 pathway, balanced inflammatory cytokines, alleviated intestinal leakage, upregulated tight junction proteins and reshaped gut microbiota by reducing Proteobacteria and enriching Firmicutes. Spearman’s correlation study indicated a strong positive relationship between Lactobacillus and Faecalibacterium with intestinal barrier function (Occludin and ZO-1) as well as antioxidant capacity, while Enterococcus was significantly and positively correlated with pro-inflammatory cytokines. These findings demonstrate that AB4-OA NPs exert pronounced protective therapeutic effects on E. coli-induced enteritis via inhibition of inflammation, attenuation of oxidative stress, protection of the intestinal barrier, and regulation of gut microbiota, and that these effects were greater than those of the corresponding physical mixture. This study proposes a novel therapeutic strategy for managing E. coli-induced enteritis and highlights the therapeutic potential of phytochemical-based self-assembled nanomedicines.
Resveratrol (RES), a natural compound widely used as a food additive and preservative, exhibits anti-inflammatory and antioxidant activities. However, its poor solubility and stability severely limit its translational potential for clinical applications. To address these challenges, we developed a core-shell nanoparticle drug delivery system (DDS) composed of zein, soy lecithin, and dextran sulfate, fabricated via a built-in ultrasonic dialysis process (BUDP). The optimized RES/ZLDS NPs exhibited uniform spherical morphology, small particle size (252.00 ± 14.64 nm), high negative zeta potential (-80.10 ± 0.66 mV), and satisfactory encapsulation efficiency (88.54 ± 1.98%) and loading capacity (7.86 ± 0.03%). Compared with free RES, RES/ZLDS NPs significantly enhanced the dissolution rate (3.90-fold), white light stability (1.41-fold), UV light stability (2.22-fold), ABTS+ scavenging activity (3.42-fold), and in vitro bioaccessibility (2.33-fold). Mechanistic studies revealed that the nanoparticles were internalized primarily via caveolae/lipid raft-mediated endocytosis, and in vivo tissue distribution demonstrated the highest RES accumulation in the lung, with approximately 2.5-fold and 2-fold increases in the heart and lung, respectively, over free RES. In an LPS-induced acute lung injury (ALI) mouse model, RES/ZLDS NPs dramatically alleviated pulmonary pathological damage and reduced IL-6 and TNF-α levels in bronchoalveolar lavage fluid by 2.79-fold and 2.45-fold, respectively, compared with free RES. Importantly, acute toxicity evaluation confirmed that RES/ZLDS NPs did not induce detectable organ damage or alter serum biochemical parameters, indicating a favorable safety profile. Collectively, our findings demonstrate that this nanoparticle system not only optimizes the physicochemical and biological performance of RES but also serves as a versatile and safe delivery platform for other food-derived bioactive compounds.
Zhen-Yao Wu, Wenqi Wu, Wu Luo et al.· International Journal of Bio...· 0 citations
