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目的用油包水乳液静电纺丝法制备并评价包载有L-肉毒碱的聚乙二醇-b-聚ε-己内酯电纺纤维毡。方法将L-肉毒碱溶解在水中为水相,将聚乙二醇与聚ε-己内酯嵌段质量比为1∶75的共聚物和1∶5的共聚物溶解在二氯甲烷中为油相,混合并超声形成W/O乳液后静电纺丝得纤维毡。扫描电子显微镜观察纤维毡形态并用图形软件进行纤维直径分布分析,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,高效液相色谱测定药物体外释放结果。结果随着油相中聚乙二醇与聚酯嵌段质量比为1∶75和1∶5两种共聚物的含量比例由高到低,纤维形状由直径较均匀的纤维向直径不均匀的纤维转变,最终形成连接珠形态,平均直径和最大直径逐渐增高。所得纤维表面光滑无结晶态物质析出,X-射线衍射没有发现L-肉毒碱特征峰出现。差示扫描量热结果显示L-肉毒碱的加入使纤维的玻璃化温度降低。随着平均直径的增高,L-肉毒碱释放速率逐渐减慢。结论采用较高相对分子质量聚酯作为成纤材料,相对分子质量较低且聚乙二醇嵌段比例较高的嵌段聚酯为乳化剂,可制得载L-肉毒碱纤维毡作为局部药物控制释放系统。
OBJECTIVE To prepare and evaluate polyethylene glycol-b-poly (ε-caprolactone) electrospun fiber mats with L-carnitine encapsulated by water-in-oil emulsion electrospinning. Methods L-carnitine was dissolved in water as an aqueous phase, a copolymer of polyethylene glycol and poly-ε-caprolactone having a mass ratio of 1: 75 and a 1: 5 copolymer were dissolved in methylene chloride For the oil phase, mixed and ultrasonic formed W / O emulsion after electrospinning the fiber mat. Scanning electron microscopy (SEM) was used to observe the morphology of the fibrous mats and the fiber diameter distribution was analyzed with a graphic software. The crystalline state of the fibers was observed by wide-angle X-ray diffraction scanning. The differential scanning calorimetry was used to evaluate the binding state of the drugs in the polymeric materials. In vitro release results. Results As the ratio of the content of polyethylene glycol to polyester block in the oil phase is 1:75 and 1: 5, the ratio of the content of the two copolymers is from high to low, and the fiber shape is from the more uniform diameter fiber to the non-uniform diameter Fiber transformation, the final formation of the connecting bead morphology, the average diameter and maximum diameter gradually increased. The resulting fiber surface without crystallization of crystalline material precipitation, X-ray diffraction did not find L-carnitine characteristic peak appears. Differential scanning calorimetry results show that the addition of L-carnitine decreases the glass transition temperature of the fiber. As the average diameter increased, L-carnitine release rate gradually slowed down. Conclusion L-carnitine fiber felt can be obtained by using relatively high molecular weight polyester as fiber-forming material and relatively low molecular weight and high content of block copolymer of polyethylene glycol as emulsifier Local Drug Controlled Release System.