Gupta Richa, Mehra Neelesh Kumar, Jain Narendra Kumar
Pharmaceutics Research Laboratory Department of Pharmaceutical Sciences, Dr. H. S. Gour University, Sagar, MP, 470 003, India.
Pharm Res. 2014 Feb;31(2):322-34. doi: 10.1007/s11095-013-1162-9. Epub 2013 Sep 17.
To develop, characterize and exploring the sulfasalazine loaded fucoyslated multi walled carbon nanotubes for Kupffer cell targeting for effective management of cytokine-induce liver damage.
Sulfasalazine was loaded into the fucosylated MWCNTs after subsequential functionalization (carboxylation, acylation and amidation) using dialysis membrane technique. The in vitro, in vivo studies were performed on macrophages J 774 cell line for Kupffer cells targeting for the treatment of cytokine-induced liver damage.
The loading of SSZ into SSZ-FUCO-MWCNTs was 87.77 ± 0.11% (n = 3). Sustained release was obtained from SSZ-FUCO-MWCNTs, with 89.12 ± 0.71% of SSZ released into medium at 48th hr. SSZ-FUCO-MWCNTs showed the 9.0 ± 0.23% hemolysis was drastically reduced from 21.62 ± 0.24% SSZMWCNTs 21.62 ± 0.24%. In SRB assay, SSZ-FUCO-MWCNTs showed more cytotoxicity than raw and SSZ-MWCNTs. In cytokine assay, SSZ- FUCO-MWCNTs exhibited significantly higher inhibition of IL-12 p40 secretion. In Western blot assay, SSZ-FUCO-MWCNTs significantly inhibit NF-κB activation.
The results suggested that the SSZ-FUCO-MWCNTs may be useful nano-carriers for targeted delivery to Kupffer cells in the treatment of cytokine-induced liver damage.
开发、表征并探索负载柳氮磺胺吡啶的岩藻糖基化多壁碳纳米管用于靶向枯否细胞，以有效管理细胞因子诱导的肝损伤。
使用透析膜技术在依次进行功能化（羧基化、酰化和酰胺化）后，将柳氮磺胺吡啶负载到岩藻糖基化的多壁碳纳米管中。对巨噬细胞J 774细胞系进行体外和体内研究，以靶向枯否细胞治疗细胞因子诱导的肝损伤。
柳氮磺胺吡啶在柳氮磺胺吡啶-岩藻糖基化多壁碳纳米管中的负载率为87.77±0.11%（n = 3）。柳氮磺胺吡啶-岩藻糖基化多壁碳纳米管实现了持续释放，在第48小时有89.12±0.71%的柳氮磺胺吡啶释放到培养基中。柳氮磺胺吡啶-岩藻糖基化多壁碳纳米管的溶血率为9.0±0.23%，与柳氮磺胺吡啶-多壁碳纳米管的21.62±0.24%相比大幅降低。在SRB试验中，柳氮磺胺吡啶-岩藻糖基化多壁碳纳米管比未处理的和柳氮磺胺吡啶-多壁碳纳米管表现出更高的细胞毒性。在细胞因子试验中，柳氮磺胺吡啶-岩藻糖基化多壁碳纳米管对IL-12 p40分泌的抑制作用显著更高。在蛋白质印迹试验中，柳氮磺胺吡啶-岩藻糖基化多壁碳纳米管显著抑制NF-κB活化。
结果表明，柳氮磺胺吡啶-岩藻糖基化多壁碳纳米管可能是用于靶向递送至枯否细胞以治疗细胞因子诱导的肝损伤的有用纳米载体。
