アスコルビルパルミテートベースの疎水性金ナノ粒子をゲムシタビン送達用ナノキャリアシステムとして開発

Breast cancer remains a major global health challenge, commonly treated with gemcitabine hydrochloride (GEM). However, GEM's short half-life and rapid metabolism limit its therapeutic efficacy. This study introduces a novel nano-drug delivery system based on gold nanoparticles (AuNPs) modified with ascorbyl palmitate (AsP) to improve GEM stability and performance. AuNPs were surface-modified via single-phase emulsification to form a hydrophobic AsP-coated nanoemulsion. Two formulations were prepared: Au-GEM-AsP-MOD (128.5 nm, - 18.3 mV, 89.5% encapsulation efficiency) and Au-GEM-AsP-Phys (106 nm, - 15.9 mV, 87% encapsulation efficiency). The Au-GEM-AsP-MOD system exhibited superior hydrophobicity, controlled GEM release (93% over 72 h), and enhanced cytotoxicity (IC₅₀ = 0.44 µg/mL) in 4T1 breast cancer cells compared with free GEM and physically adsorbed formulations. Furthermore, it maintained stability for six months under stress conditions (25 ± 2 °C, 60 ± 5% RH), indicating robustness and extended shelf life due to effective surface modification. The study highlights the synergistic effects of AsP in enhancing the therapeutic efficacy of Au-GEM-based formulations, supporting its role as a key component in combination therapy. This research lays the foundation for future development of hydrophobic nanomedical devices combining GEM and AsP for therapeutic and diagnostic applications in nanomedicine.