Effects of gold core size on regulating the performance of doxorubicin-conjugated gold nanoparticles

Studies on the influence of one critical parameter (e.g., size), targeting a specific.disease, while keeping other factors unchanged, are important for improving.understanding and application of the molecular design of biomedical nanomaterials..In this study, we used doxorubicin (Dox)-conjugated gold nanoparticles (GNPs).to investigate the effects of the size of the gold core (10, 20, or 60 nm) on the.performance of their conjugates. We found that all three conjugates differed.slightly in their physicochemical properties, facilitating a direct and accurate.assessment of the size effects of GNP-Dox conjugates on their in vitro and in vivo.performance. The cytological properties (the cell penetration rate and efficiency,.as well as the cytotoxicity) and antitumor performance (the intratumoral.penetration, treatment efficacy, and biodistribution) were highly correlated to.the size of the inorganic core. Among all test groups, although the conjugate.with a 60-nm gold core had the highest drug loading and release efficiency, the.conjugate with a 10-nm gold core displayed the best antitumor efficacy toward.the liver cancer models. This was because it showed the deepest tumor.permeability and the highest tumor cell-killing ability of Dox transported by.the relatively small GNPs. This study provides important evidence for better.understanding the effect of size on in vitro and in vivo properties of potential.therapeutic nanosystems and their structure design.

针对特定疾病，研究一个关键参数（例如尺寸）的影响，同时保持其他因素不变，对于提高对生物医学纳米材料分子设计的理解和应用非常重要。在本研究中，我们使用了与阿霉素（Dox）偶联的金纳米粒子（GNPs）来研究金核尺寸（10、20或60纳米）对其偶联物性能的影响。我们发现这三种偶联物在物理化学性质上略有不同，这有助于直接且准确地评估GNP - Dox偶联物的尺寸效应对其体外和体内性能的影响。细胞学特性（细胞穿透率和效率以及细胞毒性）和抗肿瘤性能（肿瘤内穿透、治疗效果和生物分布）与无机核的尺寸高度相关。在所有测试组中，尽管具有60纳米金核的偶联物具有最高的载药量和释放效率，但具有10纳米金核的偶联物对肝癌模型显示出最佳的抗肿瘤效果。这是因为它表现出由相对较小的GNPs运输的Dox具有最深的肿瘤渗透性和最高的肿瘤细胞杀伤能力。本研究为更好地理解尺寸对潜在治疗性纳米系统的体外和体内特性及其结构设计的影响提供了重要证据。