Wu Shichao, Yang Xiangrui, Zou Mingyuan, Hou Zhenqing, Yan Jianghua
Cancer Research Center, Medical College, Xiamen University, Xiamen, 361005, China.
Institute of Soft Matter and Biomimetics, College of Materials, Xiamen University, Xiamen, 361005, China.
Nanoscale Res Lett. 2017 Dec;12(1):416. doi: 10.1186/s11671-017-2174-x. Epub 2017 Jun 15.
Since the hydrophobic group is always essential to the synthesis of the drug-loaded nanoparticles, a majority of the methods rely heavily on organic solvent, which may not be completely removed and might be a potential threat to the patients. In this study, we completely "green" synthesized 10-hydroxycamptothecine (HCPT) loaded, folate (FA)-modified nanoneedles (HFNDs) for highly efficient cancer therapy with high drug loading, targeting property, and imaging capability. It should be noted that no organic solvent was used in the preparation process. In vitro cell uptake study and the in vivo distribution study showed that the HFNDs, with FA on the surface, revealed an obviously targeting property and entered the HeLa cells easier than the chitosan-HCPT nanoneedles without FA modified (NDs). The cytotoxicity tests illustrated that the HFNDs possessed better killing ability to HeLa cells than the individual drug or the NDs in the same dose, indicating its good anticancer effect. The in vivo anticancer experiment further revealed the pronounced anticancer effects and the lower side effects of the HFNDs. This new method without organic solvent will lead to a promising sustained drug delivery system for cancer diagnosis and treatment.
由于疏水基团对于载药纳米颗粒的合成始终至关重要,因此大多数方法严重依赖有机溶剂,而有机溶剂可能无法完全去除,并且可能对患者构成潜在威胁。在本研究中,我们完全“绿色”合成了负载10-羟基喜树碱(HCPT)、叶酸(FA)修饰的纳米针(HFNDs),用于高效癌症治疗,具有高载药量、靶向性和成像能力。需要注意的是,制备过程中未使用有机溶剂。体外细胞摄取研究和体内分布研究表明,表面带有FA的HFNDs具有明显的靶向性,比未修饰FA的壳聚糖-HCPT纳米针(NDs)更容易进入HeLa细胞。细胞毒性试验表明HFNDs在相同剂量下对HeLa细胞的杀伤能力优于单独的药物或NDs,表明其具有良好的抗癌效果。体内抗癌实验进一步揭示了HFNDs显著的抗癌效果和较低的副作用。这种不使用有机溶剂的新方法将为癌症诊断和治疗带来一个有前景的持续药物递送系统。