Hongsa Naruthai, Thinbanmai Tapanee, Luesakul Urarika, Sansanaphongpricha Kanokwan, Muangsin Nongnuj
Department of Chemistry, Faculty of Science, Chulalongkorn University, Bangkok 10330, Thailand.
National Nanotechnology Center (NANOTEC), National Science and Technology Development Agency (NSTDA), Pathum Thani 12120, Thailand.
Carbohydr Polym. 2022 Feb 1;277:118858. doi: 10.1016/j.carbpol.2021.118858. Epub 2021 Nov 4.
We report herein the development of the novel nanohybrids of gold nanoparticles reduced/stabilized/coated with collagen (AuNPs@collagen) in the first layer and subsequently modified with biotin-quat188-chitosan (Bi-QCS) in the outer layer for 5-fluorouracil (5-FU) delivery to improve cellular uptake and promote specific cell targeting of the nanocarrier. The fabrication of the layer-by-layer technique on the surface of gold nanoparticles (AuNPs) can overcome the limitation of poor drug loading capacity of the classic AuNPs from 64.67% to 87.46%. The AuNPs@collagen coated by the Bi-QCS exhibits strong electrostatic interactions between drug anion (5-FU) and amine groups of the modified chitosan as well as hydrogen bonding. Furthermore, the Bi-QCS-AuNPs@collagen demonstrated a significantly higher anti-inflammatory activity in RAW264.7 macrophage cell line. The Bi-QCS-AuNPs@collagen enhanced the activity of 5-FU approximately 3.3-fold (HeLa) and 6.2-fold (A549), compared to the free 5-Fluorouracil. According to these results, it is very promising that Bi-QCS-AuNPs@collagen can be used as an effective drug delivery carrier in the future.
我们在此报告新型纳米杂化物的研发情况，该杂化物的第一层是用胶原蛋白还原/稳定/包覆的金纳米颗粒（AuNPs@胶原蛋白），外层随后用生物素-季铵188-壳聚糖（Bi-QCS）进行修饰，用于递送5-氟尿嘧啶（5-FU），以提高细胞摄取并促进纳米载体的特异性细胞靶向。在金纳米颗粒（AuNPs）表面采用层层技术进行制备，可克服经典AuNPs药物负载能力差的局限性，将其从64.67%提高到87.46%。由Bi-QCS包覆的AuNPs@胶原蛋白在药物阴离子（5-FU）与修饰壳聚糖的胺基之间表现出强烈的静电相互作用以及氢键作用。此外，Bi-QCS-AuNPs@胶原蛋白在RAW264.7巨噬细胞系中表现出显著更高的抗炎活性。与游离的5-氟尿嘧啶相比，Bi-QCS-AuNPs@胶原蛋白使5-FU的活性提高了约3.3倍（HeLa细胞）和6.2倍（A549细胞）。根据这些结果，Bi-QCS-AuNPs@胶原蛋白未来有望用作有效的药物递送载体。
