Department of Pharmaceutics, Key Laboratory of Smart Drug Delivery, School of Pharmacy, Fudan University; Ministry of Education and PLA , Shanghai 201203 , People's Republic of China.
J Microencapsul. 2013;30(8):780-6. doi: 10.3109/02652048.2013.788086. Epub 2013 Apr 30.
Concanavalin A (ConA)-conjugated poly(ethylene glycol)-poly(lactic acid) nanoparticles (ConA-NPs) were prepared for targeted drug delivery to the cervical lymph nodes after intranasal administration. ConA, a lectin specifically binding to α-mannose and α-glucose, was covalently conjugated on NPs without loss of its carbohydrates binding bioactivity. In vitro cellular uptake experiment demonstrated that NPs could be uptaken by Calu-3 cells in a time- and concentration-dependent manner, and conjugation of ConA on NPs could significantly increase the rate and amount of cellular uptake. ConA-NP showed no obvious toxicity to Calu-3 cells in vitro or to the nasal cilia of rats in vivo. Compared with NPs without ConA, ConA-NP is more effective in targeting drugs to the deep cervical lymph nodes, as evidenced by 1.36-2.52 times increase of targeting efficiency, demonstrating that ConA-NP is a potential carrier for targeted drug delivery to the cervical lymph nodes via nasal route.
刀豆球蛋白 A（ConA）-聚乙二醇-聚乳酸纳米粒（ConA-NPs）被制备用于经鼻给药后靶向递送至颈部淋巴结。刀豆球蛋白 A 是一种特异性结合α-甘露糖和α-葡萄糖的凝集素，它在不损失其碳水化合物结合生物活性的情况下与 NPs 发生共价结合。体外细胞摄取实验表明， NPs 可以以时间和浓度依赖的方式被 Calu-3 细胞摄取，并且 ConA 与 NPs 的结合可以显著增加细胞摄取的速率和数量。ConA-NP 在体外对 Calu-3 细胞或体内对大鼠鼻纤毛均无明显毒性。与没有 ConA 的 NPs 相比，ConA-NP 更有效地将药物靶向递送至深部颈淋巴结，靶向效率增加了 1.36-2.52 倍，表明 ConA-NP 是通过鼻途径将药物靶向递送至颈部淋巴结的潜在载体。
