Lehr C M, Bouwstra J A, Kok W, Noach A B, de Boer A G, Junginger H E
Center for Bio-Pharmaceutical Sciences, Leiden University, The Netherlands.
Pharm Res. 1992 Apr;9(4):547-53. doi: 10.1023/a:1015804816582.
The possibility of developing bioadhesive drug delivery systems on the basis of molecules which selectively bind to the small intestinal epithelium by specific, receptor-mediated mechanisms was investigated using a lectin isolated from tomato fruits (Lycopersicum esculentum). The tomato lectin (TL) was found to bind specifically onto both isolated, fixed pig enterocytes and monolayers of human Caco-2 cell cultures with a similar affinity. TL-coated polystyrene microspheres (0.98 micron) also showed specific binding to enterocytes in vitro. Lectin binding was found to be favored at neutral pH and to be reduced in an acidic environment. Crude pig gastric mucin, however showed a marked cross-reactivity in vitro, indicating that lectin binding to the cell surface in vivo might be inhibited by mucus.
利用从番茄果实(番茄)中分离出的一种凝集素,研究了基于通过特定的受体介导机制选择性结合小肠上皮的分子开发生物粘附性给药系统的可能性。发现番茄凝集素(TL)以相似的亲和力特异性结合分离的固定猪肠上皮细胞和人Caco-2细胞培养单层。TL包被的聚苯乙烯微球(0.98微米)在体外也显示出与肠上皮细胞的特异性结合。发现凝集素结合在中性pH下更有利,而在酸性环境中减少。然而,粗制猪胃粘蛋白在体外显示出明显的交叉反应性,表明体内凝集素与细胞表面的结合可能被粘液抑制。