Enhancing Escin's Therapeutic Efficacy: A Nanoformulation Approach for Improved Stability and Anticancer Potential

This study explores the development of an advanced nanoformulation that integrates escin with biodegradable and non-toxic cellulose nanofibers (CNF) synthesized in our laboratory, aiming to investigate its anticancer potential benefits. The successful incorporation and uniform distribution of escin within the nanofibers were validated through a combination of UV-visible spectroscopy, Fourier-transform infrared (FTIR) spectroscopy, scanning electron microscopy, and energy-dispersive X-ray (EDX) analysis. The molecular interaction between escin and the cellulose matrix was characterized by a binding energy of -8.4 kcal/mol and a Ki of 6.88 × 10⁻⁷ M, indicating strong encapsulation with sustained release capabilities. The formulation was optimized for EE% and DL%, identifying the optimal drug-to-CNF ratio as 10:3. In vitro release studies demonstrated a controlled and prolonged release profile of escin under various pH conditions, contrasting sharply with the rapid release observed for the unencapsulated drug. The novelty of this research lies in its optimized drug loading and controlled release system, which ensures targeted, sustained action across varying pH levels, while also exhibiting selective cytotoxicity towards cancer cells and minimal effects on healthy cells. Cytotoxicity assays confirmed that the CNF-escin nanoformulation selectively targeted cancer cell lines (A549 and HepG2), exhibiting minimal toxicity towards normal cells (L132). Furthermore, the impact of the nanoformulation on cancer cell migration, mitochondrial membrane potential (MMP), ROS generation, and mitochondrial superoxide production was assessed, revealing a significant reduction in cancer cell proliferation and migration, accompanied by ROS-mediated apoptosis. These findings underscore the potential of escin-loaded cellulose nanofibers as a promising and favorable option for selectively targeting cancer.