Yin Hua Qin, Shao Guang, Gan Feng, Ye Gang
School of Chemistry, Sun Yat-Sen University, Guangzhou, 510275, People's Republic of China.
Department of Gastroenterology, the First Affiliated Hospital of Jinan University, Guangzhou, 510630, People's Republic of China.
Nanoscale Res Lett. 2020 Jan 31;15(1):29. doi: 10.1186/s11671-019-3232-3.
Gold nanoparticles (GNPs) have always been used as doxorubicin (DOX) transport vectors for tumor diagnosis and therapy; however, the synthesis process of these vectors is to prepare GNPs via chemical reduction method firstly, followed by conjugation with DOX or specific peptides, so these meth•ods faced some common problems including multiple steps, high cost, time consuming, complicated preparation, and post-processing. Here, we present a one-step strategy to prepare the DOX-conjugated GNPs on the basis of DOX's chemical constitution for the first time. Moreover, we prepare a multifunctional GNPs (DRN-GNPs) with a one-step method by the aid of the reductive functional groups possessed by DOX, RGD peptides, and nuclear localization peptides (NLS), which only needs 30 min. The results of scattering images and cell TEM studies indicated that the DRN-GNPs could target the Hela cells' nucleus. The tumor inhibition rates of DRN-GNPs via tumor and tail vein injection of nude mice were 66.7% and 57.7%, respectively, which were significantly enhanced compared to control groups. One step synthesis of multifunctional GNPs not only saves time, materials, but also it is in line with the development direction of green chemistry, and it would lay the foundation for large-scale applications within the near future. Our results suggested that the fabrication strategy is efficient, and our prepared DRN-GNPs possess good colloidal stability in the physiological system; they are a potentially contrast agent and an efficient DOX transport vector for cervical cancer diagnosis and therapy.
金纳米颗粒（GNPs）一直被用作阿霉素（DOX）的转运载体用于肿瘤诊断和治疗；然而，这些载体的合成过程是首先通过化学还原法制备GNPs，然后与DOX或特定肽进行偶联，因此这些方法面临一些常见问题，包括步骤多、成本高、耗时、制备复杂以及后处理繁琐。在此，我们首次基于DOX的化学组成提出了一种一步法策略来制备DOX偶联的GNPs。此外，借助DOX、RGD肽和核定位肽（NLS）所具有的还原官能团，我们采用一步法制备了多功能GNPs（DRN-GNPs），整个过程仅需30分钟。散射图像和细胞透射电镜研究结果表明，DRN-GNPs能够靶向Hela细胞的细胞核。通过对裸鼠进行肿瘤注射和尾静脉注射，DRN-GNPs的肿瘤抑制率分别为66.7%和57.7%，与对照组相比显著提高。多功能GNPs的一步合成不仅节省时间和材料，而且符合绿色化学的发展方向，将为在不久的将来实现大规模应用奠定基础。我们的结果表明该制备策略是有效的，并且我们制备的DRN-GNPs在生理系统中具有良好的胶体稳定性；它们是一种潜在的造影剂以及用于宫颈癌诊断和治疗的高效DOX转运载体。
