Poloxamer188复合聚L-乳酸电纺纤维中来曲唑的释放行为

Release behavior of letrozole from Poloxamer188-complexed poly L-lactic acid electrospun fibers

目的考察Poloxamer188复合聚L-乳酸电纺纤维对来曲唑的包裹和释放。方法将来曲唑、Poloxamer188和聚L-乳酸共同溶解在二氯甲烷中形成均相溶液后静电纺丝,调节Poloxamer188的复合量和来曲唑的载量。扫描电子显微镜观察产品形态,X-射线衍射、差示热分析表征三者的复合情况,高效液相色谱-紫外分光光度发法测定来曲唑的释放量,做释放曲线并回归。结果所得产品为直径均一的微米级纤维。所有纤维样品中来曲唑均被Poloxamer188增溶后释放。Poloxamer188的复合量增高有助于药物的释放,来曲唑载量的增高减慢药物的释放速率。当其含量质量分数为4.76%时,72 h后释放最大释放量的2/3以上;当其含量质量分数为13.04%时,缓释期长达6周。结论Poloxamer188复合聚L-乳酸电纺纤维体系中,Poloxamer188的复合量和来曲唑的载量对药物本身的释放行为有明显影响。

Objective To investigate letrozole incorporation in and release from Poloxamer188 complexed poly L-lactic acidelectrospun fibers.Methods Letrozole,Poloxamer188 and poly L-lactic acid were dissolved together within dichloromethane to form homogeneous solution and to be electrospun to form fibers.The morphology of fibers was characterized by scanning electron microscope.Complexation of three materials was characterized by X-ray diffraction,differential thermal analysis.Letrozole amount in release medium was determined by high performance liquid chromatography-ultra-violet spectrometry,and the release curves were drew and regressed.Results All obtained products presented as micro-scale fibers with homogeneous diameters.All fibers released letrozole after the drug was dissolving by Poloxamer188.Increasing Poloxamer188 complex amount facilitated drug release,while increasing letrozole incorporating amount slowed down drug release.Fibers presented above 2/3 release amount to maximum release amount when letrozole mass incorporating amount was 4.76%,while fibers presented more than 6 weeks sustained release when letrozole mass incorporating amount was 13.04%.Conclusion Both Poloxamer188 complexing amount and letrozoleincorporating amount have the remarkable effect on letrozole release behavior in Poloxamer188 complexed poly L-lactic acid electrospun fibers system.