A novel modified chitosan/collagen coated-gold nanoparticles for 5-fluo-rouracil delivery: Synthesis, characterization, in vitro drug release studies, anti-inflammatory activity and in vitro cytotoxicity assay

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 (BiQCS) 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-QCSAuNPs@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-QCSAuNPs@collagen can be used as an effective drug delivery carrier in the future.

Automated summary

In this study, novel nanohybrids of gold nanoparticles coated with collagen and modified with BiQCS were developed for improved drug delivery. The layer-by-layer technique increased the drug loading capacity of the nanoparticles and enhanced their cellular uptake and specific targeting. The nanohybrids also exhibited strong anti-inflammatory activity and greatly improved the activity of the drug. These findings suggest that the Bi-QCSAuNPs@collagen could be a promising drug delivery carrier in the future.