The solubilization of poorly water-soluble natural bioactive compounds remains a significant challenge. This study aims to design a ternary inclusion system to enhance the solubility of the poorly water-soluble compound Neohesperidin (NH). Soluble ternary cyclodextrin complexations (t-CDs) containing NH, 2-hydroxypropyl-β-cyclodextrin (HP-β-CD), and meglumine (MEG) were prepared and optimized. The optimized t-CDs were further characterized using Scanning Electron Microscopy (SEM), Powder X-ray Diffraction (PXRD), Differential Scanning Calorimetry (DSC), Fourier Transform Infrared Spectroscopy (FTIR), Nuclear Magnetic Resonance (NMR), and molecular docking (MD) techniques. The results suggested that NH formed was associated with MEG through hydrogen bonds with MEG, and was subsequently incorporated into the hydrophobic cavity of HP-β-CD, which may be a key factor in improving its solubility. The solubility of NH in water at 37 °C increased significantly from 0.16 mg/mL to 5.81 mg/mL in the optimized t-CDs (NH/MEG/HP-β-CD).
Neohesperidin (NH), a bioactive flavanone glycoside, exhibits multifaceted pharmacological properties including antioxidant and anti-inflammatory activities. However, its clinical application is severely constrained by inherent physicochemical limitations such as poor aqueous solubility and instability under physiological conditions. To address these challenges, this study developed a dual-carrier nano-liposomal system through the synergistic integration of phospholipid complexation and hydroxypropyl-β-cyclodextrin (HP-β-CD) inclusion technologies. Two formulations—NH-PC (phospholipid complex) and NH-PC-CD (phospholipid/HP-β-CD hybrid)—were fabricated via ultrasonication-assisted ethanol precipitation. Comprehensive characterization using FTIR and PXRD confirmed the amorphous dispersion of NH within lipid bilayers, with complete elimination of crystalline diffraction peaks, indicative of molecular-level interactions between NH’s hydroxyl groups and phospholipid polar moieties. The engineered nanosystems demonstrated remarkable solubility enhancement, achieving 321.77 μg/mL (NH-PC) and 318.75 μg/mL (NH-PC-CD), representing 2.01- and 1.99-fold increases over free NH. Encapsulation efficiencies exceeded 95% for both formulations, with sustained release profiles revealing 60.81% (NH-PC) and 80.78% (NH-PC-CD) cumulative release over 72 h, governed predominantly by non-Fickian diffusion kinetics. In vitro gastrointestinal simulations highlighted superior bioaccessibility for NH-PC-CD (66.35%) compared to NH-PC (58.52%) and free NH (20.85%), attributed to enhanced stability against enzymatic degradation. Storage stability assessments further validated the robustness of HP-β-CD-modified liposomes, with NH-PC-CD maintaining consistent particle size (92%) over 30 days. Antioxidant evaluations demonstrated concentration-dependent DPPH radical scavenging, wherein nanoencapsulation significantly amplified NH’s activity compared to its free form. This study establishes a paradigm for dual-functional nanocarriers, offering a scalable strategy to optimize the delivery of hydrophobic nutraceuticals while addressing critical challenges in bioavailability and physiological stability.
Lavender essential oil (LEO) has strong antibacterial and antioxidant properties, but its volatility limits practical use in fruit preservation. To address this limitation, we developed a pH-responsive delivery system (LEO@HZIF-8) using tannic acid (TA)-etched hollow ZIF-8 (HZIF-8) to enable controlled release of LEO. Mild etching generated a hollow structure that increased LEO encapsulation efficiency to 68.96%. Results indicate that LEO@HZIF-8 nanoparticles retain a well-defined crystalline structure and release LEO rapidly under acidic conditions, with a release rate of 73.36% at pH 4.5 after 72 h. Furthermore, LEO@HZIF-8 exhibited strong antioxidant activity, with DPPH and ABTS radical-scavenging rates of 85.48% and 78.24%, respectively, and significant antibacterial activity. When incorporated into a sodium alginate/zein (SA/Zein) coating, LEO@HZIF-8 extended the shelf life of white apricots to 63 days and effectively delayed decay, weight loss, and firmness loss. This study demonstrates an efficient pH-responsive delivery strategy for plant essential oils in freshness preservation and provides a basis for developing next-generation smart, eco-friendly active food packaging materials.
To address the volatility of lavender essential oil (LEO) in postharvest preservation, a pH-responsive delivery system was developed using tannic acid-modified hollow zeolite imidazolate framework-8 (HZIF-8) as a carrier. The hollow structure significantly enhanced the loading efficiency of LEO to 68.96%. The resulting LEO@HZIF-8 nanoparticles maintained a crystalline structure and exhibited rapid, Fickian diffusion-based release under acidic conditions. Furthermore, they demonstrated strong antioxidant activity, with DPPH and ABTS radical scavenging rates of 85.48% and 78.24%, respectively, and potent antibacterial effects, attributed to the synergy between TA and LEO. These nanoparticles were incorporated into a zein/sodium alginate composite coating. Applied to white apricots, the coating effectively extended the shelf life to 63 days by significantly reducing decay incidence, weight loss, and firmness decline. This study presents an efficient, intelligent delivery strategy for plant essential oils, contributing to the development of next-generation active and eco-friendly food packaging materials. (Word Count: 149)