载卡托普利聚(乳酸-羟基乙酸)纳米纤维毡及其释药研究

PLGA Captopril-loaded nanofibers and their in vitro release profiles

应用静电纺丝技术,以Captopril(CPL)为模型药物,以聚(乳酸-羟基乙酸)(PLGA)为载体高分子材料制备CPL/PLGA载药纳米纤维。探讨了静电纺丝工艺参数,得出最佳较优纺丝条件为原液浓度20%(质量分数),载药量:m(CPL)∶m(PLGA)=2∶10,电压12.5kV,流速1mL/h,溶剂为V(二氯甲烷)∶V(丙酮)=2∶1。应用扫描电子显微镜(SEM)、傅立叶红外光谱仪(FT-IR)、差示扫描量热仪(DSC)和采用多晶衍射仪(XRD)对所制备的载药纤维进行了表征。体外(In vitro)释药性研究实验结果表明,PLGA载药纳米纤维具有明显的初期突释,随着缓冲溶液pH值增加,初期突释减弱,药物释放度也会随之减弱。

Ultrafine captopril（CPL）-loaded poly（lactic-co-glycolic acid） （PLGA） fibers were successfully pre-pared by electrospinning method from co-dissolving solutions of PLGA and Captopril in dichloromethane （DMC） .acetone（ACT）（2 ： 1） that was made as the spinning solutions. The optimal spinning parameters wereobtained that was PLGA 20wt%, m （CPL） ： m （PLGA） = 2：10, voltage ： 12.5kV, the rate ： lmL/h, the ratio of solvent ： V（DCM） ： V（ACT）=2 ： 1. The samples thereby obtained were characterized by scanning electronmicroscopy （SEM）, Fourier transform infrared spectroscopy （FT-IR）, differential scanning caborimetry） （DSC） and X-ray diffraction （XRD） measurements. In vitro release study showed that a sustained release wasachieved after a burst release at the early stage. The burst release and overall drug was reduced as the pH ofbuffer solution increased.