炔雌醇月缓释Poloxamer188复合聚L-乳酸电纺纤维的表征

Characterization of Poloxamer188 Composite Poly L-lactic Acid Electrospun Fibers for Month Sustained Release Ethinyloestradiol

目的考察在聚L-乳酸电纺纤维体系下,Poloxamer188复合量和炔雌醇的载药量对药物包裹和释放行为的影响。方法将炔雌醇、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Poloxamer188的复合量为聚L-乳酸质量的220%、240%、260%、280%、300%,炔雌醇的载量设为聚L-乳酸质量的5%、10%、15%。扫描电子显微镜观察纤维形态,差示热分析和X-射线衍射考察材料复合状态,高效液相色谱-紫外分光光度法测定释放介质中炔雌醇的含量,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结构的纤维。炔雌醇在纤维中复合良好,Poloxamer188在纤维表面有单体存在。炔雌醇在释放全程均为被增溶状态。随着Poloxamer188复合量的增高,药物释放量增加,随着炔雌醇载量的增高,药物释放量减少。Poloxamer188复合量为300%、炔雌醇载量为5%时,药物的百分释放量接近80%,缓释期可达28 d。释放曲线能够被Peppas方程式拟合。结论Poloxamer188复合量为聚L-乳酸的220%~300%时能够得到百分释放量较高的月缓释载炔雌醇电纺纤维。

Objective To investigate the effects of Poloxamer188 composite and ethinyloestradiol loading amounts on drug encapsulation and release behavior in poly-L-lactic acid electrospinning fiber system.Methods Ethinylestradiol,Poloxamer188 and poly L-lactic acid were co-dissolved in dichloromethane to form a homogeneous solution after electrospinning,in which the recombination amount of Poloxamer188 was 220%,240%,260%,280%and 300%of the mass of poll-lactic acid.The loading of ethinylestradiol was set to 5%,10%and 15%of the mass of poly-L-lactic acid.The fiber morphology was observed by scanning electron microscope,and the composite state was investigated by differential thermal analysis and X-ray diffraction.The content of ethinylestradiol in the release medium was determined by high performance liquid chromatography-ultraviolet spectrophotometry,and the release curve was drawn and fitted.Results The obtained products are micrometer diameter uniform fiber without bead structure.Ethinylestradiol was well combined in fiber,and Poloxamer188 had monomer on fiber surface.Ethinylestradiol is solubilized in the whole process of release.With the increase of Poloxamer188 compound amount,the drug release increased,and with the increase of ethinylestradiol load,the drug release decreased.When the compound dose of Poloxamer188 was 300%and the load of ethinylestradiol was 5%,the percentage release of Poloxamer188 was close to 80%,and the sustained release period could reach 28 days.The release curve can be fitted by the Peppas equation.Conclusion When the compound amount of Poloxamer188 is 220%-300%of poly L-lactic acid,the monthly slow-release ethinylestradiol electrospun fiber with high release amount can be obtained.