Abstract:

This study aimed to optimize and characterize Idronoxil-loaded Polycaprolactone nanoparticles as a potential drug delivery system for cancer therapy, focusing on improving particle size, encapsulation efficiency, and stability using a factorial design approach. Nanoparticles were synthesized via the ionic gelation method and optimized based on PCL concentration, polyvinyl alcohol (PVA) concentration, and organic phase volume. Characterization included particle size, zeta potential, encapsulation efficiency, morphology (SEM), FT-IR analysis, in vitro drug release, and stability testing. Cytotoxicity was assessed against HepG2 liver cancer cells using the MTT assay. The optimized formulation exhibited a particle size of 97.3 nm, a zeta potential of -6.41 mV, and an encapsulation efficiency of 82.07%, ensuring stability and uniform dispersion. FT-IR confirmed the compatibility of Idronoxil with PCL. In vitro drug release studies demonstrated a controlled and sustained release profile driven by diffusion and polymer degradation, enhancing therapeutic potential. Stability testing over 90 days at 40°C±5°C validated the nanoparticles' robustness, with minimal variations in drug content and release profiles. Cytotoxicity studies demonstrated a significant dose-dependent anticancer effect on HepG2 cells, with an IC50 concentration of 19.33 µg/mL, suggesting efficient cellular uptake and potential for therapeutic use. The Idronoxil-loaded PCL nanoparticles showed excellent stability, controlled drug release, and potent anticancer activity, highlighting their potential as an effective drug delivery system for cancer therapy. Future research should focus on in vivo studies and clinical validation to establish their efficacy and safety in therapeutic applications.

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