目的:以聚己内酯/外消旋聚乳酸(PCL/PDLLA)为载体材料,制作安全有效的载有7-乙基-10-羟基喜树碱(SN-38)的缓释系统,评价对 U-251胶质瘤细胞的抗肿瘤效果。方法通过电纺丝方法制作 SN-38-PCL/PDLLA纺丝膜,采用差示扫描热分析法(DSC)及傅立叶转换红外线光谱(FTIR)分析 SN-38在载药聚合物纤维中的状态;采用接触角测量评价载药纤维的亲疏水性;在体外观察不同材料纤维的药物释放速率及对 U-251胶质瘤细胞的抑制作用。结果载药纺丝膜形态均一,在体外实验中均表现出一定的持续抑制胶质瘤细胞的能力,由于载药量的不同,表现出不同的释放时间。其中2%载药的静电纺丝膜表现出稳定、持续的抗肿瘤活性,突释不明显。结论应用 PCL/PDLLA 制备搭载 SN-38的缓释系统是可行的,适当提高载药量可以增加药物释放时间。
Objective To establisht an effectively controlled release system which was based on 7-ethyl-10-hydroxyl camptothecin (SN-38)-loaded electrospun composite nanofiber with poly (ε-caprolactone)(PCL)/poly (D,L-lac-tide)(PDLLA)and to evaluate its antitumor activity against U-251 glioma cells in vitro.Methods SN-38-loaded PCL/PDLLA fibers were manufactured by electrospinning.The physical status of SN-38 within the polymeric fibers was investigated by different scanning calorimetry (DSC)and fourier transform infrared (FT-IR).The static wettability of the membrane was measured by contact angle analyzer.The release speeds of two samples were determined,and their cytotoxicity against U-251 glioma cells was assessed in vitro.Results Uniform and smooth SN-38-loaded PCL/PDL-LA fibers were obtained.Cell toxicity test results showed that the SN-38-loaded PCL/PDLLA fibers could continuously inhibit the U-251 glioma cells.Due to different drug-loading rates,different membranes showed various release time. The antitumor activity of the 2 wt.% SN-38-loaded PCL/PDLLA nanofiber meshes were controlled and sustained. Conclusions Using SN-38-loaded composite nanofiber of PCL/PDLLA as a sustained delivery system is feasible. While the drug-loading rate is augmented,the release time of drug within the fibers will be increased accordingly.