乳液静电纺丝PLA/PEG微纳纤维膜的可控制备及负载亲疏水性药物的释放

摘要

Polylactic acid(PLA)and hydrophobic drug of camptothecin(CPT)solution play as the oil(O) phase. At the same time,gelation solution with hydrophilic drug of astragalus polysccharide(APS)play as the water(W)phase. Oil-in-water(O/W)emulsion was prepped by phase reversion method which was the method of low energy. The viscosity of O/W emulsion was adjusted by controlling the concentration and molecular weight of polyethlene glycol(PEG). The PLA/PEG micro/nano-fibers membrane was obtained by emulsion electrospun. On the one hand,the emulsion was characterized by particle size,optical microscope(OM). On the other hand, the scanning electromicroscope(SEM), infrared spectroscopy(FTIR)and X-ray diffraction (XRD)were used to characterize the structure and ingredient of the PLA/PEG micro/nano-fibers membrane. Besides,the hydrophilia and cytotoxicity test were used to evaluate the biocompatibility of PLA/PEG micro/nano-fibers membrane. In order to observe the distribution of drugs, the laser scanning confocal microscopy (CLSM)was used.The results show that different micro-nano structure of PLA/PEG micro/nano-fibers can be successful spinning by emulsion electrospun. Even though different morphology of composite membrane had different hydrophilia,but its hydrophilia was good. At the same time,PLA/PEG micro/nano-fibers membrane had a good biocompatibility with no cytotoxicity. The in vitro release results showed that the accumulative release of drugs in the phosphate buffer solution of pH=5.8 was higher than in the phosphate buffer solution of pH=6.8 and pH=7.4 so that the phosphate buffer solution of pH=5.8 was more advantageous to the release of drugs. As well as we can conclude that APS release faster than CPT. The PLA/PEG micro/nano-fibers membrane can realize differential release of drugs in phosphate buffer solution of pH=5.8.%采用低能相反转法,以聚乳酸(PLA)、疏水性药物喜树碱(CPT)溶液为油(O)相,以明胶水溶液、亲水性药物黄芪多糖(APS)为水(W)相,制备水包油(O/W)初乳液.通过控制聚乙二醇(PEG)的浓度和分子量制备O/W纺丝液,经乳液静电纺丝获得PLA/PEG微纳纤维膜.采用粒径分布、光学显微镜(OM)、扫描电子显微镜(SEM)、红外光谱(FTIR)、X射线衍射(XRD)、接触角测试和细胞毒性实验对初乳液和PLA/PEG微纳纤维膜进行表征,并通过激光共聚焦显微镜(CLSM)观察药物的分布情况.结果表明,通过乳液静电纺丝可成功制备亲水性良好的不同微纳结构的PLA/PEG微纳纤维膜.PLA/PEG微纳纤维膜形貌不同,亲水性存在差异,无细胞毒性.体外药物释放结果表明,与pH=6.8和7.4的释放介质相比,在pH=5.8的释放介质中,药物累积释放率较高,表明载药PLA/PEG微纳纤维膜能够有效减缓CPT的释放,而APS释放速率较快,可实现亲疏水性药物的差别性释放.