Bies Christiane, Lehr Claus-Michael, Woodley John F
Department of Biopharmaceutics and Pharmaceutical Technology, Saarland University, Saarbrücken, Germany.
Adv Drug Deliv Rev. 2004 Mar 3;56(4):425-35. doi: 10.1016/j.addr.2003.10.030.
The purpose of this paper is to review the history of using lectins to target and deliver drugs to their site of action. The hour of birth of "lectinology" may be defined as the description of the agglutinating properties of ricin, by Herrmann Stillmark in 1888, however, the modern era of lectinology began almost 100 years later in 1972 with the purification of different plant lectins by Sharon and Lis. The idea to use lectins for drug delivery came in 1988 from Woodley and Naisbett, who proposed the use of tomato lectin (TL) to target the luminal surface of the small intestine. Besides the targeting to specific cells, the lectin-sugar interaction can also been used to trigger vesicular transport into or across epithelial cells. The concept of bioadhesion via lectins may be applied not only for the GI tract but also for other biological barriers like the nasal mucosa, the lung, the buccal cavity, the eye and the blood-brain barrier.
本文的目的是回顾利用凝集素将药物靶向递送至其作用部位的历史。“凝集素学”的诞生时刻可定义为1888年赫尔曼·斯蒂尔马克对蓖麻毒素凝集特性的描述，然而，凝集素学的现代时代始于近100年后的1972年，当时沙龙和利斯对不同植物凝集素进行了纯化。1988年，伍德利和奈斯比特提出利用凝集素进行药物递送的想法，他们提议使用番茄凝集素（TL）靶向小肠腔表面。除了靶向特定细胞外，凝集素-糖相互作用还可用于触发囊泡转运进入或穿过上皮细胞。通过凝集素实现生物黏附的概念不仅可应用于胃肠道，还可应用于其他生物屏障，如鼻黏膜、肺、口腔、眼睛和血脑屏障。
