スマート金ナノハイブリッドの迅速かつグリーンな放射線誘起合成と、効果的な抗がん剤送達システムのためのカチオン性プルランによる機能化

Herein, this study presents for the first time a rapid and green radiation-induced synthesis of smart gold nanohybrids stabilized/capped/functionalized with cationic pullulan (GNHs@C-PUL) for 5Fu delivery, aiming to improve intracellular uptake, efficacy, and safety of anticancer drugs. The systematically optimized synthesis condition for controlling the morphology and particle size of multifunctional GNHs@C-PUL were identified as pH = 8 with 1.5 %(w/v) C-PUL and a gamma radiation dose of 2 kGy. The pH-responsive GNHs@C-PUL were fully characterized and exhibited a spherical shape with a homogeneous particle size of approximately 6.88 ± 1.95 nm. 5Fu was successfully loaded onto spherical GNHs@C-PUL to form newly formulated 5Fu-GNHs@C-PUL (10.10 ± 2.94 nm) via intermolecular interactions, exhibiting a faster release rate under acidic conditions (pH 5.3) with 72.86 % released over 48 h. Interestingly, the self-assembled 5Fu-GNHs@C-PUL (IC₅₀ = 47.85 μM) exhibited efficient intracellular uptake via endocytosis and enhanced the anticancer activity of 5Fu against MCF7 cells by up to 4.94-time compared to free 5Fu (IC₅₀ = 236.20 μM). Moreover, this system also induced cell cycle arrest at the G0-G1 phase by 11.33 % and substantially increased the proportion of total apoptotic cells by 30.15 % compared to free 5Fu. These results suggest that the newly developed 5Fu-GNHs@C-PUL can be considered a promising candidate nanocarrier for effective anticancer drug delivery systems.