ArticleNanomaterials (Basel, Switzerland)2025
Phospholipid/HP-β-CD Hybrid Nanosystems Amplify Neohesperidin Bioavailability via Dual Enhancement of Solubility and Stability.
Article in Nanomaterials (Basel, Switzerland), 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.
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Abstract
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 (<3% variation) and encapsulation efficiency (>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.
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