摘要
目的考察在Poloxamer188复合聚L-乳酸电纺纤维体系下,多西紫杉醇载量对其本身释放行为的影响。方法将多西紫杉醇、Poloxamer188、聚L-乳酸共同溶解在二氯甲烷中形成均相溶液后静电纺丝,其中多西紫杉醇的复合量设为占聚L-乳酸质量的10%、15%、20%、25%。扫描电子显微镜观察纤维形态,高效液相色谱-紫外分光光度发法测定水释放介质中多西紫杉醇的含量,绘制释放曲线并拟合。结果所得产品均为微米级直径均匀无珠子的纤维。当多西紫杉醇的载量为10%和15%时,百分释放率略有上升,释放初期有微晶出现、随后为溶解状态,释放曲线能够被Korsmeyer-Peppas方程式拟合,多西紫杉醇的载量为20%和25%时,百分释放率迅速下降,全部释放期均为微晶状态,释放曲线能够被零级方程式拟合。结论 Poloxamer188复合聚L-乳酸电纺纤维对多西紫杉醇的释放能力有限,多西紫杉醇载量超过Poloxamer188增溶能力时其绝对释放量并无增加。
Objective To investigate the effect of docetaxel load on its release in Poloxamer188 complexed poly L-lactic acid electrospun fibers. Method Docetaxel,Poloxamer188 and poly L-lactic acid were dissolved in dichloromethane to form homogeneous solution and prepared for electrospinning. The content of docetaxel was set at 10%,5%,20%,and 25% in poly L-lactic acid. The morphology of the fibers was observed by scanning electron microscope. The content of docetaxel in the release medium of water was determined by high performance liquid chromatography-ultra-violet spectrometry,and the release curves were drew and fitted. Results All the products were beadles fibers with uniform micron diameter. When the load of docetaxel was 10% and 15%,the percentage release rate increased a little. Some microcrystals appeared in the medium at the beginning and thereafter dissolved,and the release curves could be fitted by Korsmeyer-Peppas’ equation. When the load of docetaxel was 20% and 25%,the percentage release rate decreased rapidly. The medium turned to be micro-crystals during the whole release process,and the release curves could be fitted by0-order equation. Conclusions Poloxamer188 complexed poly L-lactic acid electrospun fibers has limited ability to release docetaxel. The absolute release hardly increases when the load of docetaxel exceeds the dissolving ability of Poloxamer188.
作者
张天
刘阳
罗徐
程博闻
王浩
Zhang Tian;LIU Yang;Luo Xu;Cheng Bowen;Wang Hao(School of Pharmaceutical Science,Jinzhou Medical University,Jinzhou,Liaoning 121000 China;Key Laboratory of Medical Macromolecules of Shandong Province,Academy of Pharmaceutical Sciences of Shandong Province,Ji nan 250014 China;Graduate School,Tianjin University of Science and Technology,Tianjin 300457 China)
出处
《锦州医科大学学报》
CAS
2019年第5期1-7,I0001-I0003,共10页
Journal of Jinzhou Medical University
基金
辽宁省药物作用与质量评价工程技术中心主任基金项目(2018110605)
2018年度山东省药学科学院山东省医用高分子材料重点实验室科研平台开放课题(2017GSF18168)
中国博士后基金资助项目(2014M561187)
辽宁省大学生创新基金项目(201710160000228)