聚L-乳酸与聚乙二醇-b-聚L-乳酸电纺纤维中布洛芬的释放

Ibuprofen release from poly (L-lactic acid) and PEG blocked poly (L-lactic acid) electrospun fibers

目的制备并评价包载有布洛芬的聚L-乳酸和聚乙二醇嵌段聚L-乳酸电纺纤维毡。方法静电纺丝法制备包载布洛芬的纤维毡,扫描电子显微镜观察纤维形态,广角X射线衍射扫描观察纤维表面结晶状态,差示扫描量热评价药物在高分子材料中的结合状态。高效液相色谱测定体外酶降解药物释放结果。结果纤维直径在0.3～1.5μm之间,表面光滑无结晶态物质析出,X射线衍射没有发现布洛芬特征峰出现。差示扫描量热结果显示布洛芬的加入使纤维的玻璃化温度降低。药物释放结果显示相对于纯聚乳酸材料,当载体材料为聚乙二醇嵌段的聚乳酸时,纤维中的布洛芬呈现更快的释放速率,聚乙二醇有利于释放介质中酶对纤维的作用。20%载药量纤维中的药物释放速率大于10%载药量纤维中的药物释放速率,蛋白酶K加快药物的释放速率。结论成功制得布洛芬电纺纤维,药物被较好包裹在纤维内部,聚乳酸电纺纤维中聚乙二醇嵌段对布洛芬释放行为有明显的影响,需要在进一步研究中注意。

Objective To prepare and evaluate poly L-lactic acid and polyethylene glycol blocked poly L-lactic acid electrospun fibrous mats with ibuprofen entrapped.Methods Fiber mats with ibuprofen entrapped were prepared by electrospinning and observed by ESEM.Fibers surface was scanned by WAXD and drug-polymer material composition state was evaluated by DSC.HPLC was used for determining the drug release result in vitro by emzyme degradation.Results Diameters of fibers were generally from 0.3-1.5 μm.Surfaces of all fibers were smooth without crytalline substances.Characteristic peaks of ibuprofen were not found.DSC detection indicated that addition of ibuprofen into fibers made the glass transition temperature lower.Ibuprofen exhibited more rapid release rate when it was entrapped in PEG-PLLA fibers than in PLLA fibers and it was suggested that PEG segment facilitated proteinase K to exert its effect on fibers.High ibuprofen loading amount was also a factor facilitated the release rate of the drug itself from fibers.According drug release profile analysis,the drug release rate for fibers with 20% drug loading amount was higher than that for fibers with 10% ibuprofen load.Proteinase K in release media had significant effect for speeding drug release rate.Conclusions Electrospun fibrous mats is successfully prepared with ibuprofen perfectly entrapped in inner fibers.Polyethylene glycol block has significant effect on ibuprofen release behavior that entrapped in poly lactic acid electrospun fibers,which should be paid attention to in future research.