Duncan R, Kopecek J, Rejmanová P, Lloyd J B
Biochim Biophys Acta. 1983 Feb 22;755(3):518-21. doi: 10.1016/0304-4165(83)90258-1.
Soluble synthetic polymers have potential as targetable carriers of pharmacological agents. Here we report that incorporation into poly[N-(2-hydroxypropyl)methacrylamide)] of an oligopeptide side-chain terminating in galactose enhanced the polymer's pinocytic uptake from the rat bloodstream by the liver. Within the liver lysosomes enzymic digestion led to the intracellular release of a drug analogue also bound to oligopeptide side-chains of the polymer.
可溶性合成聚合物有潜力作为药物的靶向载体。在此我们报告,在聚[N-(2-羟丙基)甲基丙烯酰胺]中引入以半乳糖结尾的寡肽侧链,增强了聚合物从大鼠血液循环中被肝脏通过胞饮作用摄取的能力。在肝脏溶酶体内,酶促消化导致与聚合物寡肽侧链相连的药物类似物在细胞内释放。