Seki Toshinobu, Fukushi Nanako, Chono Sumio, Morimoto Kazuhiro
Hokkaido Pharmaceutical University School of Pharmacy, 7-1 Katsuraoka-cho, Otaru, Hokkaido 047-0264, Japan.
J Control Release. 2008 Feb 11;125(3):246-51. doi: 10.1016/j.jconrel.2007.10.017. Epub 2007 Oct 26.
Sperminated pullulans (SP) and gelatin (SG) having different numbers of amino groups were prepared as sperminated polymers for absorption enhancement and the absorption-enhancing effects on the pulmonary absorption of insulin in rats and the permeation of FITC-dextran (MW 4400, FD4) through Calu-3 cell monolayers were evaluated. In both in vivo and in vitro experimental systems, SP and SG acted as enhancers and their enhancing effects correlated with the amino group content. The zeta potential of red blood cells treated with SP and SG was positive and the degree was also correlated with the amino group content. SP and SG interact directly with the luminal surface of mucus membranes via an ion-ion interaction and then may induce signals that open tight junctions resulting in intercellular permeation of water soluble drugs.
制备了具有不同氨基数量的发芽支链淀粉（SP）和明胶（SG）作为发芽聚合物用于增强吸收，并评估了它们对大鼠肺部胰岛素吸收以及荧光素异硫氰酸酯 - 葡聚糖（MW 4400，FD4）透过Calu - 3细胞单层的渗透增强作用。在体内和体外实验系统中，SP和SG均作为增强剂，其增强作用与氨基含量相关。用SP和SG处理的红细胞的ζ电位为正，且程度也与氨基含量相关。SP和SG通过离子 - 离子相互作用直接与粘膜腔表面相互作用，然后可能诱导打开紧密连接的信号，从而导致水溶性药物的细胞间渗透。
