Poloxamer188复合聚L-乳酸电纺纤维中己烯雌酚和阿那曲唑的释放行为

Release behavior of diethylstilbestrol and anastrozole from Poloxamer188-complexed poly L-lactic acid electrospun fibers

目的考察己烯雌酚和阿那曲唑从Poloxamer188复合聚L-乳酸电纺纤维中的释放行为。方法将药物与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。扫描电子显微镜观察产品形态,X-射线衍射和傅里叶变换红外光谱表征药物-Poloxamer188的复合情况,高效液相色谱-紫外分光光度法测定药物的释放量并做释放曲线。考察了Poloxamer188的复合量为12.5%、25%、50%、75%、100%和载药量为10%、20%、30%时的情形。结果两种药物的系列纤维均为微米级纤维,大体上随着Poloxamer188复合量的增高,纤维的直径变大。当载药量固定时,随着Poloxamer188复合量的增高,两种药物的百分释放量均逐渐增高。当Poloxamer188复合量固定时,随着载药量由10%增加至20%和30%,己烯雌酚的百分释放量逐渐减小,而阿那曲唑的百分释放量逐渐增加。结论Poloxamer188复合聚L-乳酸电纺纤维体系中,Poloxamer188的复合量和药物载量对药物本身的释放行为有明显影响。

Objective To investigate diethylstilbestrol and anastrozole incorporation in and release from Poloxamer188 complexed poly L-lactic acid electrospun fibers.Methods Drug,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 drug and Poloxamer188 was characterized by X-ray diffraction and Fourier transform infrared spectroscopy.Drug amount in release medium was determined by high performance liquid chromatography-ultra-violet spectrometry,and the release curves were drew.Situations of Poloxamer188 complexing amounts of 12.5%,25%,50%,75%,100%and drug loading amounts of 10%,20%and 30%were investigated.Results All obtained products presented as micro-scale fibers.Generally,with the increase of Poloxamer188 compound amount,the diameter of the fiber became larger.When the drug loading amounts were fixed,with the increase of the compound amount of Poloxamer188,the percentage release of the two drugs gradually increased.When Poloxamer188 complexing amounts were fixed,as drugs loading amounts increased from 10%to 20%and 30%,the release percentages of diethylstilbestrol decreased,while the release percentages of anastrozole increased.Conclusion Both Poloxamer188 complexing amount and drug incorporating amount have a marked effect on drug release behavior in Poloxamer188 complexed poly L-lactic acid electrospun fibers system.