乙交酯丙交酯共聚物电纺丝超细纤维对利福平的控制释放

Release of Rifampin from poly(lactide-co-glycolide) electrospun fiber mats

载药电纺丝超细纤维体系是药物控制释放领域中一个全新的剂型,近年来已引起广泛的关注。研究了乙交酯丙交酯共聚物(PLGA,LA/GA=80/20)电纺丝超细纤维在磷酸盐缓冲液(pH=7.4)中对利福平的控制释放行为。结果显示利福平的释放过程可分为2个阶段:在第一阶段为释放慢速期,药物的释放速率取决于纤维中利福平分子的扩散速率;第二阶段为释放快速期,纤维的水解速率成为控制药物释放速率的主导因素。第一阶段释放时间的长短取决于纤维中利福平的担载量,同时,还受其他因素影响,如缓冲液中表面活性剂的加入。在第二阶段,由于PLGA载体的水解可被其水解产物(乳酸和羟基乙酸)催化,因此利福平的释放表现出自加速的趋势,尤其在后期释放速率很快。

Drug-containing electrospun fiber mat is a promising controlled release formulation,and great progress has been made recently.In this article,the release behavior of Rifampin from poly（lactide-co-glycolide）（PLGA,LA/GA=80/20） electrospun fibers in phosphate buffer solution（pH 7.4） was examined.The results showed that the release process of Rifampin is divided into the early stage and the late stage.In the early stage,the drug release is determined by the diffusion of the Rifampin molecules in fibers,and in the late stage,the hydrolysis becomes the determining factor for the drug release.The length of the early stage depends on Rifampin content in the fibers and on other factors,such as surfactants and their content in the buffer solution.Because the hydrolysis of PLGA carrier is catalyzed by the hydrolysis products lactic acid and glycolic acid,the Rifampin release exhibits a tendency of acceleration and the release rate becomes quite fast in the late stage.