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<p>This study reports the development and in vitro evaluation of aescin-loaded cellulose nanocrystals (A-CNC) as a nanocarrier system for the improved delivery of aescin. The optimized formulation, prepared at a drug-to-carrier ratio of 10:3, achieved high encapsulation efficiency (&gt; 85%) with a drug loading of ~ 10%. In cytotoxicity assays, A-CNC exhibited IC₅₀ of 21.11&#xa0;µg/ml in A549 and 7.56&#xa0;µg/ml in HepG2 cells, while normal L132 cells showed a much higher IC₅₀ (88.64&#xa0;µg/ml), confirming reduced off-target toxicity compared to free aescin (IC₅₀ ~ 11–16&#xa0;µg/ml across all cell lines). Apoptosis assays revealed that A-CNC induced apoptosis in A549 (~55%) and HepG2 (~68%) cells, associated with elevated intracellular ROS (~ 85%) and significant mitochondrial membrane potential loss (~ 70%). Fluorescence-based assays (Hoechst/PI staining, ROS quantification, MMP analysis, and wound-healing assays) supported the enhanced bioactivity of A-CNC. Release studies demonstrated a sustained, pH-responsive profile, with greater stability under mildly acidic conditions. Physicochemical characterization using ultraviolet–visible spectroscopy, Fourier transform infrared spectroscopy, dynamic light scattering, scanning electron microscopy, and energy-dispersive X-ray analysis confirmed successful encapsulation, nanoscale stability, and drug–carrier interactions. Collectively, these findings indicate that CNCs can act as efficient in vitro carriers for aescin, improving its delivery, stability, and selective cytotoxicity. Further in vivo studies will be required to validate therapeutic relevance.</p> Graphical Abstract <p>Enzyme-Derived CNC Nanocarriers for Targeted Aescin Delivery and Cancer Cell Apoptosis</p> <p></p>

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Aescin-Cellulose Nanocrystals for the Enhancement of Oxidative Damage, Mitochondrial Dysfunction, and Anti-migratory Potential in Cancer Cells

  • 期刊论文

  • 发表日期：

    2026年4月8日

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  • Richa Seth,
  • Anurag Mathur,
  • Mahima Raj,
  • Abha Meena

摘要

This study reports the development and in vitro evaluation of aescin-loaded cellulose nanocrystals (A-CNC) as a nanocarrier system for the improved delivery of aescin. The optimized formulation, prepared at a drug-to-carrier ratio of 10:3, achieved high encapsulation efficiency (> 85%) with a drug loading of ~ 10%. In cytotoxicity assays, A-CNC exhibited IC₅₀ of 21.11 µg/ml in A549 and 7.56 µg/ml in HepG2 cells, while normal L132 cells showed a much higher IC₅₀ (88.64 µg/ml), confirming reduced off-target toxicity compared to free aescin (IC₅₀ ~ 11–16 µg/ml across all cell lines). Apoptosis assays revealed that A-CNC induced apoptosis in A549 (~55%) and HepG2 (~68%) cells, associated with elevated intracellular ROS (~ 85%) and significant mitochondrial membrane potential loss (~ 70%). Fluorescence-based assays (Hoechst/PI staining, ROS quantification, MMP analysis, and wound-healing assays) supported the enhanced bioactivity of A-CNC. Release studies demonstrated a sustained, pH-responsive profile, with greater stability under mildly acidic conditions. Physicochemical characterization using ultraviolet–visible spectroscopy, Fourier transform infrared spectroscopy, dynamic light scattering, scanning electron microscopy, and energy-dispersive X-ray analysis confirmed successful encapsulation, nanoscale stability, and drug–carrier interactions. Collectively, these findings indicate that CNCs can act as efficient in vitro carriers for aescin, improving its delivery, stability, and selective cytotoxicity. Further in vivo studies will be required to validate therapeutic relevance.

Graphical Abstract

Enzyme-Derived CNC Nanocarriers for Targeted Aescin Delivery and Cancer Cell Apoptosis