Poloxamer188复合载多西紫杉醇聚L-乳酸电纺纤维的制备及表征

Preparation and characterization of Poloxamer188-complexed docetaxel-incorporated poly L-lactic acid electrospun fibers

目的考察均相纺丝条件下,Poloxamer188复合量对聚L-乳酸电纺纤维中多西紫杉醇释放的影响。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。采用扫描电子显微镜观察纤维形态,X-射线衍射、差示热分析、傅里叶变换红外光谱表征三者的符合情况,采用高效液相色谱-紫外分光光度发法测定水释放介质中多西紫杉醇的含量,绘制释放曲线并采用Freundlich方程式进行拟合。结果 Poloxamer188的复合量越高,多西紫杉醇的突释量和14 d后的释放量越高,突释部分为混悬微晶,缓释部分为澄清溶液。Poloxamer188的复合量在60%以上时,能够得到无珠子、直径较为均一的纤维,纤维表面有结晶态的Poloxamer188存在;Poloxamer188的复合量达到70%以上时,释放曲线有明显的缓释相;Poloxamer188的复合量为100%时,多西紫杉醇的相对释放百分率达到58%。多西紫杉醇的释放曲线可用Freundlich方程式进行拟合。结论多西紫杉醇-Poloxamer188-聚L-乳酸均相溶液电纺复合纤维中,Poloxamer188促进了多西紫杉醇的释放。

Objective To investigate the effect of Poloxamer188 complexing amount to release of docetaxel which was incorporated within poly L-lactic acid homogeneous solution-electrospun fibers. Methods Docetaxel,Poloxamer188 and poly L-lactic acid were dissolved 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 and Fourier transform infrared spectrum. Docetaxel amount in water release medium was determined by high performance liquid chromatography-ultra-violet spectrometry,and the release curves were drewand regressed. Results No-beads fibers of homogeneous diameters could be obtained when the complexing amount of Poloxamer188 was above 60%,there was Poloxamer188 of crystalline state existing on the fibers surface. The more Poloxamer188 complexing amounts were,the more burst release amount and after 14 d release amount were. Burst released docetaxel were crystalline suspensions while the sustained released docetaxel were transparent solutions. When Poloxamer188 complexing amount was above 70%,there became to be obvious sustained release phase. When Poloxamer188 complexing amount was 100%,the relative percentage release ratio could be 58%. Docetaxel release curves could be regressed by Freundlich’s equation. Conclusion Poloxamer188 facilitated the release of docetaxel in docetaxel-poloxamer188-poly lactic acid homogeneous solution electrospun fibers。