Kim J E, Kim S R, Lee S H, Lee C H, Kim D D
College of Pharmacy, Pusan National University, 609-735, Pusan, South Korea.
Int J Pharm. 2000 May 15;201(1):29-36. doi: 10.1016/s0378-5173(00)00388-4.
The effect of various pore formers on the controlled release of an antibacterial agent from a polymeric device was examined in order to develop a novel biomaterial that prevents bacterial adhesion and growth on its surface. Cefadroxil was chosen as the model antibiotic and was incorporated into a polyurethane matrix by the solvent-casting method. Polyethylene glycol (PEG) 1450, D-mannitol, or bovine serum albumin (BSA) was used as a pore former. The amount of cefadroxil released from various formulations at 37 degrees C was measured by HPLC. The morphological change of matrices before and after release studies was investigated by scanning electron microscopy (SEM). The duration of antimicrobial activities of matrices against Escherichia coli and Bacillus subtilis was evaluated by measuring the diameters of the inhibition zone. Changing the weight fraction and particle size of the pore formers/drug mixtures could control the release of cefadroxil from the matrix. The release rate of cefadroxil increased as the loading dose of the pore former increased (15<20<25%). Cefadroxil released from these devices exhibited antibacterial activity for 5-6 days. These results imply that an antibiotic-loaded polymeric device that could prevent bacterial infection on its surface can be formulated using appropriate pore formers.
为开发一种能防止细菌在其表面粘附和生长的新型生物材料，研究了各种成孔剂对聚合物装置中抗菌剂控释的影响。选择头孢羟氨苄作为模型抗生素，并通过溶剂浇铸法将其掺入聚氨酯基质中。聚乙二醇（PEG）1450、D-甘露醇或牛血清白蛋白（BSA）用作成孔剂。通过高效液相色谱法测定37℃下从各种制剂中释放的头孢羟氨苄的量。通过扫描电子显微镜（SEM）研究释放研究前后基质的形态变化。通过测量抑菌圈直径评估基质对大肠杆菌和枯草芽孢杆菌的抗菌活性持续时间。改变成孔剂/药物混合物的重量分数和粒径可以控制头孢羟氨苄从基质中的释放。头孢羟氨苄的释放速率随着成孔剂负载量的增加而增加（15%<20%<25%）。从这些装置中释放的头孢羟氨苄表现出5至6天的抗菌活性。这些结果表明，使用合适的成孔剂可以制备一种能防止其表面细菌感染的载抗生素聚合物装置。
