Thongborisute Jringjai, Takeuchi Hirofumi
Department of Pharmaceutical Engineering, Gifu Pharmaceutical University, 5-6-1 Mitahora-Higashi, Gifu 502-8585, Japan.
Int J Pharm. 2008 Apr 16;354(1-2):204-9. doi: 10.1016/j.ijpharm.2007.12.001. Epub 2007 Dec 7.
To evaluate the reliability of the BIACORE method as a useful method for measuring the mucoadhesive interaction between chitosan and mucin, the mucin-particle method was used for comparison. In this study, the adhesivities of different-molecular-weight chitosans (chitosan Mw. 150,000, CS; low-molecular-weight chitosan, LCS) and hydrophobically modified chitosans (dodecylated CS, d-CS; dodecylated LCS, d-LCS) to mucin were determined. The BIACORE method showed that CS, LCS and d-CS could interact with mucin based on the increased resonance unit (RU) response after mucin was passed over the chitosans-immobilized sensor chip surface. Sensorgrams obtained from the interaction between these polymers and mucin also indicated the rate and strength of binding reaction. The rate and strength were higher for unmodified chitosans than hydrophobically modified chitosans. The simple in vitro mucoadhesive test or mucin-particle method revealed that the turbidity of unmodified chitosan/mucin mixtures was higher than that of dodecylated chitosans for all concentration of chitosans and mucin. The results from both BIACORE and the mucin-particle method implied that hydrophobic modification of chitosan reduced its adhesivity to mucin. The results from these two methods corresponded well. Therefore, the BIACORE method has promised as an alternative method for evaluating the adhesivity of adhesive polymers to mucin.
为评估生物传感器（BIACORE）方法作为测量壳聚糖与粘蛋白之间粘膜粘附相互作用的有用方法的可靠性，采用粘蛋白颗粒法进行比较。在本研究中，测定了不同分子量壳聚糖（壳聚糖Mw. 150,000，CS；低分子量壳聚糖，LCS）和疏水改性壳聚糖（十二烷基化CS, d-CS；十二烷基化LCS, d-LCS）对粘蛋白的粘附性。BIACORE方法表明，当粘蛋白通过固定有壳聚糖的传感器芯片表面后，基于共振单位（RU）响应的增加，CS、LCS和d-CS可与粘蛋白相互作用。从这些聚合物与粘蛋白之间相互作用获得的传感图也表明了结合反应的速率和强度。未改性壳聚糖的结合速率和强度高于疏水改性壳聚糖。简单的体外粘膜粘附试验或粘蛋白颗粒法显示，对于所有壳聚糖和粘蛋白浓度，未改性壳聚糖/粘蛋白混合物的浊度高于十二烷基化壳聚糖。BIACORE和粘蛋白颗粒法的结果均表明壳聚糖的疏水改性降低了其对粘蛋白的粘附性。这两种方法的结果吻合良好。因此，BIACORE方法有望成为评估粘附性聚合物对粘蛋白粘附性的替代方法。
